EOS Med Chem, Medicinal Chemical is Big is China TOP 100 CRO comapny, mainly in Med-chemicals, Custom synthesis. We have GMP, ISO plant plant serving you.
EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.
EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.
2018 CHINA CPHI, W4E82
EOS Med Chem, Medchem is Big 執大象，天下往，往而無害，安平泰 WEB: www.eosmedchem.com EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com TEL: 0086-531-69905422 GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: MS049 is a potent and selective inhibitor of PRMT4,6 and is active in cells.
Name: MS049
CAS#: 1502816-23-0
Chemical Formula: C15H24N2O
Exact Mass: 248.1889
Molecular Weight: 248.37
Elemental Analysis: C, 72.54; H, 9.74; N, 11.28; O, 6.44
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
REFERENCES
1: Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, de Freitas RF, Senisterra G, Li F, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Oct 13;59(19):9124-9139. doi: 10.1021/acs.jmedchem.6b01033. Epub 2016 Sep 15. PubMed PMID: 27584694; PubMed Central PMCID: PMC5063716.
EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.
EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.
2018 CHINA CPHI, W4E82
EOS Med Chem, Medchem is Big 執大象，天下往，往而無害，安平泰 WEB: www.eosmedchem.com EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com TEL: 0086-531-69905422 GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: CD437 is a synthetic retinoid that is an RARγ-selective agonist. It displays RARγ-dependent and -independent effects on differentiation and apoptosis.
Name: CD437
CAS#: 125316-60-1
Chemical Formula: C27H26O3
Exact Mass: 398.1882
Molecular Weight: 398.5
Elemental Analysis: C, 81.38; H, 6.58; O, 12.04
Synonym: CD437; CD 437; CD-437; Ro-472077; Ro 472077; Ro472077; AHPN.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
REFERENCES
1: Han T, Goralski M, Capota E, Padrick SB, Kim J, Xie Y, Nijhawan D. The antitumor toxin CD437 is a direct inhibitor of DNA polymerase α. Nat Chem Biol. 2016 Jul;12(7):511-5. doi: 10.1038/nchembio.2082. Epub 2016 May 16. PubMed PMID: 27182663; PubMed Central PMCID: PMC4912453.
2: Magnussen GI, Ree Rosnes AK, Shahzidi S, Dong HP, Emilsen E, Engesæter B, Flørenes VA. Synthetic retinoid CD437 induces apoptosis and acts synergistically with TRAIL receptor-2 agonist in malignant melanoma. Biochem Biophys Res Commun. 2012 Apr 13;420(3):516-22. doi: 10.1016/j.bbrc.2012.03.023. Epub 2012 Mar 13. PubMed PMID: 22446330.
3: Mishur RJ, Griffin ME, Battle CH, Shan B, Jayawickramarajah J. Molecular recognition and enhancement of aqueous solubility and bioactivity of CD437 by β-cyclodextrin. Bioorg Med Chem Lett. 2011 Jan 15;21(2):857-60. doi: 10.1016/j.bmcl.2010.11.073. Epub 2010 Nov 21. PubMed PMID: 21185186; PubMed Central PMCID: PMC3057113.
4: Hashiguchi K, Tsuchiya H, Tomita A, Ueda C, Akechi Y, Sakabe T, Kurimasa A, Nozaki M, Yamada T, Tsuchida S, Shiota G. Involvement of ETS1 in thioredoxin-binding protein 2 transcription induced by a synthetic retinoid CD437 in human osteosarcoma cells. Biochem Biophys Res Commun. 2010 Jan 1;391(1):621-6. doi: 10.1016/j.bbrc.2009.11.109. Epub 2009 Nov 20. PubMed PMID: 19932085.
5: Matsuoka S, Tsuchiya H, Sakabe T, Watanabe Y, Hoshikawa Y, Kurimasa A, Itamochi H, Harada T, Terakawa N, Masutani H, Yodoi J, Shiota G. Involvement of thioredoxin-binding protein 2 in the antitumor activity of CD437. Cancer Sci. 2008 Dec;99(12):2485-90. doi: 10.1111/j.1349-7006.2008.00979.x. Epub 2008 Nov 17. PubMed PMID: 19018770.
6: Pan M, Geng S, Xiao S, Ren J, Liu Y, Li X, Li Z, Peng Z. Apoptosis induced by synthetic retinoic acid CD437 on human melanoma A375 cells involves RIG-I pathway. Arch Dermatol Res. 2009 Jan;301(1):15-20. doi: 10.1007/s00403-008-0902-x. Epub 2008 Oct 21. PubMed PMID: 18936944.
7: Valli C, Paroni G, Di Francesco AM, Riccardi R, Tavecchio M, Erba E, Boldetti A, Gianni' M, Fratelli M, Pisano C, Merlini L, Antoccia A, Cenciarelli C, Terao M, Garattini E. Atypical retinoids ST1926 and CD437 are S-phase-specific agents causing DNA double-strand breaks: significance for the cytotoxic and antiproliferative activity. Mol Cancer Ther. 2008 Sep;7(9):2941-54. doi: 10.1158/1535-7163.MCT-08-0419. PubMed PMID: 18790775.
8: Gonda K, Tsuchiya H, Sakabe T, Akechi Y, Ikeda R, Nishio R, Terabayashi K, Ishii K, Matsumi Y, Ashla AA, Okamoto H, Takubo K, Matsuoka S, Watanabe Y, Hoshikawa Y, Kurimasa A, Shiota G. Synthetic retinoid CD437 induces mitochondria-mediated apoptosis in hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2008 Jun 13;370(4):629-33. doi: 10.1016/j.bbrc.2008.04.008. Epub 2008 Apr 10. PubMed PMID: 18406343.
9: Pan M, Peng ZH, Xiao SX, Li XL, Liu Y, Li ZX, Ren JW. [A novel retinoid CD437 induces apoptosis of human epidermoid carcinoma A431 cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2008 Mar;28(3):305-8. Chinese. PubMed PMID: 18359678.
10: Watanabe Y, Tsuchiya H, Sakabe T, Matsuoka S, Akechi Y, Fujimoto Y, Yamane K, Ikeda R, Nishio R, Terabayashi K, Ishii K, Gonda K, Matsumi Y, Ashla AA, Okamoto H, Takubo K, Tomita A, Hoshikawa Y, Kurimasa A, Itamochi H, Harada T, Terakawa N, Shiota G. CD437 induces apoptosis in ovarian adenocarcinoma cells via ER stress signaling. Biochem Biophys Res Commun. 2008 Feb 15;366(3):840-7. Epub 2007 Dec 17. PubMed PMID: 18082618.
11: Jiang T, Soprano DR, Soprano KJ. GADD45A is a mediator of CD437 induced apoptosis in ovarian carcinoma cells. J Cell Physiol. 2007 Sep;212(3):771-9. PubMed PMID: 17474084.
12: Parrella E, Giannì M, Fratelli M, Barzago MM, Raska I Jr, Diomede L, Kurosaki M, Pisano C, Carminati P, Merlini L, Dallavalle S, Tavecchio M, Rochette-Egly C, Terao M, Garattini E. Antitumor activity of the retinoid-related molecules (E)-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926) and 6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid (CD437) in F9 teratocarcinoma: Role of retinoic acid receptor gamma and retinoid-independent pathways. Mol Pharmacol. 2006 Sep;70(3):909-24. Epub 2006 Jun 20. PubMed PMID: 16788091.
13: Zou C, Zhou J, Qian L, Feugang JM, Liu J, Wang X, Wu S, Ding H, Zou C, Liebert M, Grossman HB. Comparing the effect of ATRA, 4-HPR, and CD437 in bladder cancer cells. Front Biosci. 2006 Sep 1;11:2007-16. PubMed PMID: 16720286.
14: Jin F, Liu X, Zhou Z, Yue P, Lotan R, Khuri FR, Chung LW, Sun SY. Activation of nuclear factor-kappaB contributes to induction of death receptors and apoptosis by the synthetic retinoid CD437 in DU145 human prostate cancer cells. Cancer Res. 2005 Jul 15;65(14):6354-63. PubMed PMID: 16024638.
15: Boisvieux-Ulrich E, Sourdeval M, Marano F. CD437, a synthetic retinoid, induces apoptosis in human respiratory epithelial cells via caspase-independent mitochondrial and caspase-8-dependent pathways both up-regulated by JNK signaling pathway. Exp Cell Res. 2005 Jul 1;307(1):76-90. Epub 2005 Apr 18. PubMed PMID: 15922728.
16: Kim HJ, Lotan R. Identification of protein modulation by the synthetic retinoid CD437 in lung carcinoma cells using high throughput immunoblotting. Int J Oncol. 2005 Feb;26(2):483-91. PubMed PMID: 15645134.
17: Holmes WF, Soprano DR, Soprano KJ. Early events in the induction of apoptosis in ovarian carcinoma cells by CD437: activation of the p38 MAP kinase signal pathway. Oncogene. 2003 Sep 25;22(41):6377-86. PubMed PMID: 14508518.
18: Rishi AK, Zhang L, Boyanapalli M, Wali A, Mohammad RM, Yu Y, Fontana JA, Hatfield JS, Dawson MI, Majumdar AP, Reichert U. Identification and characterization of a cell cycle and apoptosis regulatory protein-1 as a novel mediator of apoptosis signaling by retinoid CD437. J Biol Chem. 2003 Aug 29;278(35):33422-35. Epub 2003 Jun 18. PubMed PMID: 12816952.
19: Holmes WF, Soprano DR, Soprano KJ. Comparison of the mechanism of induction of apoptosis in ovarian carcinoma cells by the conformationally restricted synthetic retinoids CD437 and 4-HPR. J Cell Biochem. 2003 May 15;89(2):262-78. PubMed PMID: 12704790.
20: Joseph B, Marchetti P, Lefebvre O, Schraen-Maschke S, Méreau-Richard C, Formstecher P. The novel retinoid AHPN/CD437 induces a rapid but incomplete apoptotic response in human myeloma cells. Biochim Biophys Acta. 2003 Feb 17;1593(2-3):277-82. PubMed PMID: 12581872.
EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.
EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.
2018 CHINA CPHI, W4E82
EOS Med Chem, Medchem is Big 執大象，天下往，往而無害，安平泰 WEB: www.eosmedchem.com EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com TEL: 0086-531-69905422 GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: Ilomastat, also known as GM6001 and galardin, is a broad-spectrum matrix metalloproteinase inhibitor with potential anticancer activity. GM6001 is a member of the hydroxamic acid class of reversible metallopeptidase inhibitors. The anionic state of the hydroxamic acid group forms a bidentate complex with the active site zinc. Examples of enzymes that ilomastat inhibit include thermolysin, peptide deformylase, and anthrax lethal factor endopeptidase (LF) produced by the bacterium Bacillus anthracis.
Name: Ilomastat
CAS#: 142880-36-2
Chemical Formula: C20H28N4O4
Exact Mass: 388.21106
Molecular Weight: 388.46072
Elemental Analysis: C, 61.84; H, 7.27; N, 14.42; O, 16.47
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
ADDITIONAL INFORMATION
REFERENCES
1: Bencsik P, Pálóczi J, Kocsis GF, Pipis J, Belecz I, Varga ZV, Csonka C, Görbe A, Csont T, Ferdinandy P. Moderate inhibition of myocardial matrix metalloproteinase-2 by ilomastat is cardioprotective. Pharmacol Res. 2014 Feb;80:36-42. doi: 10.1016/j.phrs.2013.12.007. Epub 2013 Dec 28. PubMed PMID: 24380772.
2: Parkinson G, Gaisford S, Ru Q, Lockwood A, Khalili A, Sheridan R, Khaw PT, Brocchini S, Fadda HM. Characterisation of ilomastat for prolonged ocular drug release. AAPS PharmSciTech. 2012 Dec;13(4):1063-72. doi: 10.1208/s12249-012-9832-1. Epub 2012 Aug 18. PubMed PMID: 22903888; PubMed Central PMCID: PMC3513442.
3: Senhao L, Dongqin Q. Preparation and in vitro evaluation of an ilomastat microemulsion gel by a self-microemulsifying system. Pharmazie. 2012 Feb;67(2):156-60. PubMed PMID: 22512086.
4: Yeh DY, Lin HI, Feng NH, Chen CF, Wang D, Wang NT. Matrix metalloprotease expressions in both reperfusion lung injury and oleic acid lung injury models and the protective effects of ilomastat. Transplant Proc. 2009 Jun;41(5):1508-11. doi: 10.1016/j.transproceed.2009.02.076. PubMed PMID: 19545667.
5: Wang YD, Wang W. Protective effect of ilomastat on trinitrobenzenesulfonic acid-induced ulcerative colitis in rats. World J Gastroenterol. 2008 Oct 7;14(37):5683-8. PubMed PMID: 18837084; PubMed Central PMCID: PMC2748202.
7: Moroy G, Denhez C, El Mourabit H, Toribio A, Dassonville A, Decarme M, Renault JH, Mirand C, Bellon G, Sapi J, Alix AJ, Hornebeck W, Bourguet E. Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies. Bioorg Med Chem. 2007 Jul 15;15(14):4753-66. Epub 2007 May 6. PubMed PMID: 17512742.
8: Kocer SS, Walker SG, Zerler B, Golub LM, Simon SR. Metalloproteinase inhibitors, nonantimicrobial chemically modified tetracyclines, and ilomastat block Bacillus anthracis lethal factor activity in viable cells. Infect Immun. 2005 Nov;73(11):7548-57. PubMed PMID: 16239558; PubMed Central PMCID: PMC1273843.
9: Wong TT, Mead AL, Khaw PT. Prolonged antiscarring effects of ilomastat and MMC after experimental glaucoma filtration surgery. Invest Ophthalmol Vis Sci. 2005 Jun;46(6):2018-22. PubMed PMID: 15914618.
10: Antonelli PJ, Schultz GS, Sundin DJ, Pemberton PA, Barr PJ. Protease inhibitors alpha1-antitrypsin and ilomastat are not ototoxic in the chinchilla. Laryngoscope. 2003 Oct;113(10):1764-9. PubMed PMID: 14520103.
11: Antonelli PJ, Schultz GS, Kim KM, Cantwell JS, Sundin DJ, Pemberton PA, Barr PJ. Alpha 1-antitrypsin and ilomastat inhibit inflammatory proteases present in human middle ear effusions. Laryngoscope. 2003 Aug;113(8):1347-51. PubMed PMID: 12897557.
EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.
EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.
2018 CHINA CPHI, W4E82
EOS Med Chem, Medchem is Big 執大象，天下往，往而無害，安平泰 WEB: www.eosmedchem.com EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com TEL: 0086-531-69905422 GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorectic effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes.
Name: SB-334867 free base
CAS#: 792173-99-0 (free base)
Chemical Formula: C17H13N5O2
Exact Mass: 319.1069
Molecular Weight: 319.324
Elemental Analysis: C, 63.94; H, 4.10; N, 21.93; O, 10.02
Related CAS #: 792173-99-0 (free base) 249889-64-3 (HCl)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
REFERENCES
1: Hooshmand B, Azizi H, Javan M, Semnanian S. Intra-LC microinjection of orexin type-1 receptor antagonist SB-334867 attenuates the expression of glutamate-induced opiate withdrawal like signs during the active phase in rats. Neurosci Lett. 2017 Jan 1;636:276-281. doi: 10.1016/j.neulet.2016.10.051. Epub 2016 Nov 2. PubMed PMID: 27816550.
2: Kordi Jaz E, Moghimi A, Fereidoni M, Asadi S, Shamsizadeh A, Roohbakhsh A. SB-334867, an orexin receptor 1 antagonist, decreased seizure and anxiety in pentylenetetrazol-kindled rats. Fundam Clin Pharmacol. 2017 Apr;31(2):201-207. doi: 10.1111/fcp.12249. Epub 2016 Nov 23. PubMed PMID: 27739093.
3: Mayannavar S, Rashmi KS, Rao YD, Yadav S, Ganaraja B. Effect of Orexin A antagonist (SB-334867) infusion into the nucleus accumbens on consummatory behavior and alcohol preference in Wistar rats. Indian J Pharmacol. 2016 Jan-Feb;48(1):53-8. doi: 10.4103/0253-7613.174528. PubMed PMID: 26997723; PubMed Central PMCID: PMC4778208.
4: Socała K, Szuster-Ciesielska A, Wlaź P. SB 334867, a selective orexin receptor type 1 antagonist, elevates seizure threshold in mice. Life Sci. 2016 Apr 1;150:81-8. doi: 10.1016/j.lfs.2016.02.075. Epub 2016 Feb 23. PubMed PMID: 26916826.
5: Vanderhaven MW, Cornish JL, Staples LG. The orexin-1 receptor antagonist SB-334867 decreases anxiety-like behavior and c-Fos expression in the hypothalamus of rats exposed to cat odor. Behav Brain Res. 2015 Feb 1;278:563-8. doi: 10.1016/j.bbr.2014.10.028. Epub 2014 Oct 30. PubMed PMID: 25447305.
6: Staples LG, Cornish JL. The orexin-1 receptor antagonist SB-334867 attenuates anxiety in rats exposed to cat odor but not the elevated plus maze: an investigation of Trial 1 and Trial 2 effects. Horm Behav. 2014 Mar;65(3):294-300. doi: 10.1016/j.yhbeh.2013.12.014. Epub 2014 Jan 4. PubMed PMID: 24397997.
7: Azhdari-Zarmehri H, Esmaeili MH, Sofiabadi M, Haghdoost-Yazdi H. Orexin receptor type-1 antagonist SB-334867 decreases morphine-induced antinociceptive effect in formalin test. Pharmacol Biochem Behav. 2013 Nov;112:64-70. doi: 10.1016/j.pbb.2013.09.018. Epub 2013 Oct 12. PubMed PMID: 24125787.
8: McElhinny CJ Jr, Lewin AH, Mascarella SW, Runyon S, Brieaddy L, Carroll FI. Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6661-4. doi: 10.1016/j.bmcl.2012.08.109. Epub 2012 Sep 7. PubMed PMID: 23031594.
9: Ranjbar-Slamloo Y, Azizi H, Fathollahi Y, Semnanian S. Orexin receptor type-1 antagonist SB-334867 inhibits the development of morphine analgesic tolerance in rats. Peptides. 2012 May;35(1):56-9. doi: 10.1016/j.peptides.2012.02.023. Epub 2012 Mar 6. PubMed PMID: 22421510.
10: Rusyniak DE, Zaretsky DV, Zaretskaia MV, Durant PJ, DiMicco JA. The orexin-1 receptor antagonist SB-334867 decreases sympathetic responses to a moderate dose of methamphetamine and stress. Physiol Behav. 2012 Dec 5;107(5):743-50. doi: 10.1016/j.physbeh.2012.02.010. Epub 2012 Feb 14. PubMed PMID: 22361264; PubMed Central PMCID: PMC3371311.
11: Putula J, Kukkonen JP. Mapping of the binding sites for the OX1 orexin receptor antagonist, SB-334867, using orexin/hypocretin receptor chimaeras. Neurosci Lett. 2012 Jan 6;506(1):111-5. doi: 10.1016/j.neulet.2011.10.061. Epub 2011 Nov 2. PubMed PMID: 22079339.
12: Perrey DA, Gilmour BP, Runyon SP, Thomas BF, Zhang Y. Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists. Bioorg Med Chem Lett. 2011 May 15;21(10):2980-5. doi: 10.1016/j.bmcl.2011.03.048. Epub 2011 Mar 21. PubMed PMID: 21478014; PubMed Central PMCID: PMC3085582.
13: Jupp B, Krivdic B, Krstew E, Lawrence AJ. The orexin₁ receptor antagonist SB-334867 dissociates the motivational properties of alcohol and sucrose in rats. Brain Res. 2011 May 19;1391:54-9. doi: 10.1016/j.brainres.2011.03.045. Epub 2011 Mar 23. PubMed PMID: 21439948.
14: Mediavilla C, Cabello V, Risco S. SB-334867-A, a selective orexin-1 receptor antagonist, enhances taste aversion learning and blocks taste preference learning in rats. Pharmacol Biochem Behav. 2011 May;98(3):385-91. doi: 10.1016/j.pbb.2011.01.021. Epub 2011 Feb 2. PubMed PMID: 21295056.
15: Hutcheson DM, Quarta D, Halbout B, Rigal A, Valerio E, Heidbreder C. Orexin-1 receptor antagonist SB-334867 reduces the acquisition and expression of cocaine-conditioned reinforcement and the expression of amphetamine-conditioned reward. Behav Pharmacol. 2011 Apr;22(2):173-81. doi: 10.1097/FBP.0b013e328343d761. PubMed PMID: 21285875.
16: Dhaher R, Hauser SR, Getachew B, Bell RL, McBride WJ, McKinzie DL, Rodd ZA. The Orexin-1 Receptor Antagonist SB-334867 Reduces Alcohol Relapse Drinking, but not Alcohol-Seeking, in Alcohol-Preferring (P) Rats. J Addict Med. 2010 Sep;4(3):153-9. doi: 10.1097/ADM.0b013e3181bd893f. PubMed PMID: 20871792; PubMed Central PMCID: PMC2943642.
17: Quarta D, Valerio E, Hutcheson DM, Hedou G, Heidbreder C. The orexin-1 receptor antagonist SB-334867 reduces amphetamine-evoked dopamine outflow in the shell of the nucleus accumbens and decreases the expression of amphetamine sensitization. Neurochem Int. 2010 Jan;56(1):11-5. doi: 10.1016/j.neuint.2009.08.012. Epub 2009 Sep 6. PubMed PMID: 19737591.
18: Boschen KE, Fadel JR, Burk JA. Systemic and intrabasalis administration of the orexin-1 receptor antagonist, SB-334867, disrupts attentional performance in rats. Psychopharmacology (Berl). 2009 Oct;206(2):205-13. doi: 10.1007/s00213-009-1596-2. Epub 2009 Jul 3. PubMed PMID: 19575184.
19: Jochem J. Orexin type 1 receptor antagonist SB 334867 inhibits the central histamine-induced resuscitating effect in rats subjected to haemorrhagic shock. Inflamm Res. 2009 Apr;58 Suppl 1:36-7. doi: 10.1007/s00011-009-0657-7. PubMed PMID: 19271123.
20: Nair SG, Golden SA, Shaham Y. Differential effects of the hypocretin 1 receptor antagonist SB 334867 on high-fat food self-administration and reinstatement of food seeking in rats. Br J Pharmacol. 2008 May;154(2):406-16. doi: 10.1038/bjp.2008.3. Epub 2008 Jan 28. PubMed PMID: 18223663; PubMed Central PMCID: PMC2442445.
EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.
EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.
2018 CHINA CPHI, W4E82
EOS Med Chem, Medchem is Big 執大象，天下往，往而無害，安平泰 WEB: www.eosmedchem.com EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com TEL: 0086-531-69905422 GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: Upadacitinib, also known as ABT-494, is a potent and selective JAK inhibitors in development for rheumatoid arthritis. ABT-494 is approximately 74 fold selective for Jak1 over Jak2 in cellular assays dependent on specific, relevant cytokines. ABT-494 demonstrates efficacy in rat arthritis models. Preliminary evidence suggests that compared to tofacitinib, ABT-494 may spare Jak2 and Jak3 dependent signaling.
Name: Upadacitinib
CAS#: 1310726-60-3 (free base)
Chemical Formula: C17H19F3N6O
Exact Mass: 380.1572
Molecular Weight: 380.3752
Elemental Analysis: C, 53.68; H, 5.04; F, 14.98; N, 22.09; O, 4.21
Related CAS #: 1310726-60-3 (free base) 1607431-21-9 (tartarte)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
REFERENCES
1: Genovese MC, Smolen JS, Weinblatt ME, Burmester GR, Meerwein S, Camp HS, Wang L, Othman AA, Khan N, Pangan AL, Jungerwirth S. Efficacy and Safety of ABT-494, a Selective JAK-1 Inhibitor, in a Phase IIb Study in Patients With Rheumatoid Arthritis and an Inadequate Response to Methotrexate. Arthritis Rheumatol. 2016 Dec;68(12):2857-2866. doi: 10.1002/art.39808. PubMed PMID: 27390150; PubMed Central PMCID: PMC5132065.
2: Kremer JM, Emery P, Camp HS, Friedman A, Wang L, Othman AA, Khan N, Pangan AL, Jungerwirth S, Keystone EC. A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy. Arthritis Rheumatol. 2016 Dec;68(12):2867-2877. doi: 10.1002/art.39801. PubMed PMID: 27389975; PubMed Central PMCID: PMC5132116.
3: Mohamed MF, Camp HS, Jiang P, Padley RJ, Asatryan A, Othman AA. Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Subjects with Rheumatoid Arthritis. Clin Pharmacokinet. 2016 Dec;55(12):1547-1558. PubMed PMID: 27272171.
5: Nakayamada S, Kubo S, Iwata S, Tanaka Y. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419. Review. Erratum in: BioDrugs. 2016 Oct;30(5):483. PubMed PMID: 27577235.
6: Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Review. PubMed PMID: 24818516.
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Description: HMN-176 is an active metabolite of the synthetic antitumor compound HMN-214. HMN-176 shows potent cytotoxicity toward various human tumor cell lines, and in mitotic cells, it causes cell cycle arrest at M phase through the destruction of spindle polar bodies, followed by the induction of DNA fragmentation. However, no direct interactions of HMN-176 with tubulin are observed. Moreover, in animal models, it was observed that oral administration of the prodrug HMN-214 caused no significant nerve toxicity, a severe side effect often associated with microtubule binding agents such as Taxol and VCR.3 In Phase I clinical trials, HMN-214 has caused sensory neuropathy and ileus in some patients. However, the grade and frequency of these adverse effects were much lower than those of typical microtubule binding agents. As expected from the mechanism of action of HMN-214 (induction of G2-M arrest in dividing cells), the main adverse effect was neutropenia. (Source: CANCER RESEARCH 63, 6942–6947).
Name: HMN-176
CAS#: 173529-10-7
Chemical Formula: C20H18N2O4S
Exact Mass: 382.09873
Molecular Weight: 382.43
Elemental Analysis: C, 62.81; H, 4.74; N, 7.33; O, 16.73; S, 8.38
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
ADDITIONAL INFORMATION
HMN-176 is a potential new cancer therapeutic known to retard the proliferation of tumor cell lines. This compound inhibits meiotic spindle assembly in surf clam oocytes and delays satisfaction of the spindle assembly checkpoint in human somatic cells by inducing the formation of short and/or multipolar spindles. HMN-176 does not affect centrosome assembly, nuclear envelope breakdown, or other aspects of meiotic or mitotic progression, nor does it affect the kinetics of Spisula or mammalian microtubule (MT) assembly in vitro. Notably, HMN-176 inhibits the formation of centrosome-nucleated MTs (i.e., asters) in Spisula oocytes and oocyte extracts, as well as from isolated Spisula or mammalian centrosomes in vitro. Together, these results reveal that HMN-176 is a first-in-class anticentrosome drug that inhibits proliferation, at least in part, by disrupting centrosome-mediated MT assembly during mitosis. (source: Mol Cancer Ther. 2009 Mar;8(3):592-601. ).
REFERENCES
1: DiMaio MA, Mikhailov A, Rieder CL, Von Hoff DD, Palazzo RE. The small organic compound HMN-176 delays satisfaction of the spindle assembly checkpoint by inhibiting centrosome-dependent microtubule nucleation. Mol Cancer Ther. 2009 Mar;8(3):592-601. doi: 10.1158/1535-7163.MCT-08-0876. Epub 2009 Mar 3. PubMed PMID: 19258425; PubMed Central PMCID: PMC2717217.
2: Garland LL, Taylor C, Pilkington DL, Cohen JL, Von Hoff DD. A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors. Clin Cancer Res. 2006 Sep 1;12(17):5182-9. PubMed PMID: 16951237.
3: Medina-Gundrum L, Cerna C, Gomez L, Izbicka E. Investigation of HMN-176 anticancer activity in human tumor specimens in vitro and the effects of HMN-176 on differential gene expression. Invest New Drugs. 2005 Jan;23(1):3-9. PubMed PMID: 15528975.
4: Takagi M, Honmura T, Watanabe S, Yamaguchi R, Nogawa M, Nishimura I, Katoh F, Matsuda M, Hidaka H. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest New Drugs. 2003 Nov;21(4):387-99. PubMed PMID: 14586206.
5: Tanaka H, Ohshima N, Ikenoya M, Komori K, Katoh F, Hidaka H. HMN-176, an active metabolite of the synthetic antitumor agent HMN-214, restores chemosensitivity to multidrug-resistant cells by targeting the transcription factor NF-Y. Cancer Res. 2003 Oct 15;63(20):6942-7. PubMed PMID: 14583495.
