Original: S107 free base 927871-76-9, stock more than 100g

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: S107 is a Type 1 ryanodine receptor (RyR1) stabilizer; binds RyR1 and enhances the binding affinity of calstabin-1. Inhibits Ca leak from the sarcoplasmic reticulum (SR).

Name: S107 free base 

CAS#: 927871-76-9 (free base) 

Chemical Formula: C11H15NOS 

Exact Mass: 209.0874 

Molecular Weight: 209.307 

Elemental Analysis: C, 63.12; H, 7.22; N, 6.69; O, 7.64; S, 15.32

Related CAS #: 1357476-46-0 (HCl)   927871-76-9 (free base)    

Synonym: S107; S-107; S 107.

IUPAC/Chemical Name: 2,3,4,5-Tetrahydro-7-methoxy-4-methyl-1,4-benzothiazepine

InChi Key: BGVCEGVSQDOGSB-UHFFFAOYSA-N

InChi Code: InChI=1S/C11H15NOS/c1-12-5-6-14-11-4-3-10(13-2)7-9(11)8-12/h3-4,7H,5-6,8H2,1-2H3

SMILES Code: CN1CCSC2=CC=C(OC)C=C2C1

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: Mei Y, Xu L, Kramer HF, Tomberlin GH, Townsend C, Meissner G. Stabilization of the skeletal muscle ryanodine receptor ion channel-FKBP12 complex by the 1,4-benzothiazepine derivative S107. PLoS One. 2013;8(1):e54208. doi: 10.1371/journal.pone.0054208. Epub 2013 Jan 17. PubMed PMID: 23349825; PubMed Central PMCID: PMC3547879.

2: Kreko-Pierce T, Azpurua J, Mahoney RE, Eaton BA. Extension of Health Span and Life Span in Drosophila by S107 Requires the calstabin Homologue FK506-BP2. J Biol Chem. 2016 Dec 9;291(50):26045-26055. Epub 2016 Nov 1. PubMed PMID: 27803160; PubMed Central PMCID: PMC5207075.

3: Sasaki K, Makiyama T, Yoshida Y, Wuriyanghai Y, Kamakura T, Nishiuchi S, Hayano M, Harita T, Yamamoto Y, Kohjitani H, Hirose S, Chen J, Kawamura M, Ohno S, Itoh H, Takeuchi A, Matsuoka S, Miura M, Sumitomo N, Horie M, Yamanaka S, Kimura T. Patient-Specific Human Induced Pluripotent Stem Cell Model Assessed with Electrical Pacing Validates S107 as a Potential Therapeutic Agent for Catecholaminergic Polymorphic Ventricular Tachycardia. PLoS One. 2016 Oct 20;11(10):e0164795. doi: 10.1371/journal.pone.0164795. eCollection 2016. PubMed PMID: 27764147; PubMed Central PMCID: PMC5072719.

4: Beuck S, Schänzer W, Thevis M. Investigation of the in vitro metabolism of the emerging drug candidate S107 for doping-preventive purposes. J Mass Spectrom. 2011 Feb;46(2):112-30. doi: 10.1002/jms.1878. Epub 2011 Jan 21. PubMed PMID: 21254313.

5: Ahmed MA, De Avila M, Polverini E, Bessonov K, Bamm VV, Harauz G. Solution nuclear magnetic resonance structure and molecular dynamics simulations of a murine 18.5 kDa myelin basic protein segment (S72-S107) in association with dodecylphosphocholine micelles. Biochemistry. 2012 Sep 25;51(38):7475-87. doi: 10.1021/bi300998x. Epub 2012 Sep 14. PubMed PMID: 22947219.

6: Pennell CA. Selection for S107-V11 gene expression by peritoneal B cells in adult mice. J Immunol. 1995 Aug 1;155(3):1264-75. PubMed PMID: 7636194.

7: Fowler JF Jr. Facial Dermatitis and Rosacea. Semin Cutan Med Surg. 2016 Jun;35(6 Suppl):S107-9. doi: 10.12788/j.sder.2016.034. PubMed PMID: 27537212.

8: White R, Tran TA, Dankenbring CA, Deaton J, Young R. The N-terminal transmembrane domain of lambda S is required for holin but not antiholin function. J Bacteriol. 2010 Feb;192(3):725-33. doi: 10.1128/JB.01263-09. Epub 2009 Nov 6. PubMed PMID: 19897658; PubMed Central PMCID: PMC2812449.

9: Baumann B, Kistler B, Kirillov A, Bergman Y, Wirth T. The mutant plasmacytoma cell line S107 allows the identification of distinct pathways leading to NF-kappaB activation. J Biol Chem. 1998 May 8;273(19):11448-55. PubMed PMID: 9565556.

10: Cary S, Krishnan M, Marion TN, Silverman GJ. The murine clan V(H) III related 7183, J606 and S107 and DNA4 families commonly encode for binding to a bacterial B cell superantigen. Mol Immunol. 1999 Aug;36(11-12):769-76. PubMed PMID: 10593515.

11: Shan J, Xie W, Betzenhauser M, Reiken S, Chen BX, Wronska A, Marks AR. Calcium leak through ryanodine receptors leads to atrial fibrillation in 3 mouse models of catecholaminergic polymorphic ventricular tachycardia. Circ Res. 2012 Aug 31;111(6):708-17. doi: 10.1161/CIRCRESAHA.112.273342. Epub 2012 Jul 24. PubMed PMID: 22828895; PubMed Central PMCID: PMC3734386.

12: Steiner M, Bläsi U. Charged amino-terminal amino acids affect the lethal capacity of Lambda lysis proteins S107 and S105. Mol Microbiol. 1993 May;8(3):525-33. PubMed PMID: 8326864.

13: Graschopf A, Bläsi U. Molecular function of the dual-start motif in the lambda S holin. Mol Microbiol. 1999 Aug;33(3):569-82. PubMed PMID: 10417647.

14: Jiang Y, Khan FA, Pandupuspitasari NS, Kadariya I, Cheng Z, Ren Y, Chen X, Zhou A, Yang L, Kong D, Zhang S. Analysis of the binding sites of porcine sialoadhesin receptor with PRRSV. Int J Mol Sci. 2013 Dec 9;14(12):23955-79. doi: 10.3390/ijms141223955. PubMed PMID: 24351868; PubMed Central PMCID: PMC3876088.

15: Deaton J, Savva CG, Sun J, Holzenburg A, Berry J, Young R. Solubilization and delivery by GroEL of megadalton complexes of the lambda holin. Protein Sci. 2004 Jul;13(7):1778-86. PubMed PMID: 15215521; PubMed Central PMCID: PMC2279943.

16: Kwan SP, Max EE, Seidman JG, Leder P, Scharff MD. Two kappa immunoglobulin genes are expressed in the myeloma S107. Cell. 1981 Oct;26(1 Pt 1):57-66. PubMed PMID: 6799208.

17: Stewart GA, Turner KJ. Physicochemical and immunochemical characterization of the high molecular weight allergens from dermatophagoides pteronysisinus with particular reference to the tridacnin, Con-A and S107 reactive components. Aust J Exp Biol Med Sci. 1980 Jun;58(3):275-88. PubMed PMID: 7458776.

18: Yeh LC, Falcon WE, Garces A, Lee JC, Lee JC. A host-guest relationship in bone morphogenetic protein receptor-II defines specificity in ligand-receptor recognition. Biochemistry. 2012 Sep 4;51(35):6968-80. doi: 10.1021/bi3003023. Epub 2012 Aug 23. PubMed PMID: 22894880; PubMed Central PMCID: PMC3481545.

19: Liu M, Lee DF, Chen CT, Yen CJ, Li LY, Lee HJ, Chang CJ, Chang WC, Hsu JM, Kuo HP, Xia W, Wei Y, Chiu PC, Chou CK, Du Y, Dhar D, Karin M, Chen CH, Hung MC. IKKα activation of NOTCH links tumorigenesis via FOXA2 suppression. Mol Cell. 2012 Jan 27;45(2):171-84. doi: 10.1016/j.molcel.2011.11.018. Epub 2011 Dec 22. PubMed PMID: 22196886; PubMed Central PMCID: PMC3268914.

20: Giusti AM, Chien NC, Zack DJ, Shin SU, Scharff MD. Somatic diversification of S107 from an antiphosphocholine to an anti-DNA autoantibody is due to a single base change in its heavy chain variable region. Proc Natl Acad Sci U S A. 1987 May;84(9):2926-30. PubMed PMID: 3106981; PubMed Central PMCID: PMC304773.

Original: BAY41-4109 racemic 298708-79-9, stock more than 100g

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: BAY41-4109 racemic is a mixture of R-isomer of BAY41-4109 and S-isomer of BAY41-4109. BAY-41-4109 is a heteroaryldihydropyrimidine (HAP) antiviral compound effective on Hepatitis B virus (HBV) capsid assembly and on preformed HBV capsids.

Name: BAY41-4109 racemic 

CAS#: 298708-79-9 (racemic) 

Chemical Formula: C18H13ClF3N3O2 

Exact Mass: 395.0648 

Molecular Weight: 395.7662 

Elemental Analysis: C, 54.63; H, 3.31; Cl, 8.96; F, 14.40; N, 10.62; O, 8.09

Related CAS #: 298708-79-9 (racemic)   298708-81-3 (R-isomer)    

Synonym: BAY-41-4109; BAY41-4109; BAY 41-4109; BAY-414109; BAY414109; BAY 414109.

IUPAC/Chemical Name: Methyl 4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoropyridin-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate

InChi Key: FVNJBPMQWSIGJK-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H13ClF3N3O2/c1-8-14(18(26)27-2)15(11-4-3-9(20)5-12(11)19)25-17(24-8)16-13(22)6-10(21)7-23-16/h3-7,15H,1-2H3,(H,24,25)

SMILES Code: O=C(C1=C(C)NC(C2=NC=C(F)C=C2F)=NC1C3=CC=C(F)C=C3Cl)OC

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: Wu G, Liu B, Zhang Y, Li J, Arzumanyan A, Clayton MM, Schinazi RF, Wang Z, Goldmann S, Ren Q, Zhang F, Feitelson MA. Preclinical characterization of GLS4, an inhibitor of hepatitis B virus core particle assembly. Antimicrob Agents Chemother. 2013 Nov;57(11):5344-54. doi: 10.1128/AAC.01091-13. Epub 2013 Aug 19. PubMed PMID: 23959305; PubMed Central PMCID: PMC3811253.

2: Brezillon N, Brunelle MN, Massinet H, Giang E, Lamant C, DaSilva L, Berissi S, Belghiti J, Hannoun L, Puerstinger G, Wimmer E, Neyts J, Hantz O, Soussan P, Morosan S, Kremsdorf D. Antiviral activity of Bay 41-4109 on hepatitis B virus in humanized Alb-uPA/SCID mice. PLoS One. 2011;6(12):e25096. doi: 10.1371/journal.pone.0025096. Epub 2011 Dec 5. PubMed PMID: 22162746; PubMed Central PMCID: PMC3230577.

3: Billioud G, Pichoud C, Puerstinger G, Neyts J, Zoulim F. The main hepatitis B virus (HBV) mutants resistant to nucleoside analogs are susceptible in vitro to non-nucleoside inhibitors of HBV replication. Antiviral Res. 2011 Nov;92(2):271-6. doi: 10.1016/j.antiviral.2011.08.012. Epub 2011 Aug 18. PubMed PMID: 21871497.

4: Wu GY, Zheng XJ, Yin CC, Jiang D, Zhu L, Liu Y, Wei L, Wang Y, Chen HS. Inhibition of hepatitis B virus replication by Bay 41-4109 and its association with nucleocapsid disassembly. J Chemother. 2008 Aug;20(4):458-67. PubMed PMID: 18676226.

5: Pan XB, Han JC, Wei L, Peng DD, Gao Y. [Subcellular distribution and translocation of hepatitis B virus core protein in HepG2.2.15 cells]. Zhonghua Gan Zang Bing Za Zhi. 2008 Jan;16(1):29-32. Chinese. PubMed PMID: 18226340.

6: Shi C, Wu CQ, Cao AM, Sheng HZ, Yan XZ, Liao MY. NMR-spectroscopy-based metabonomic approach to the analysis of Bay41-4109, a novel anti-HBV compound, induced hepatotoxicity in rats. Toxicol Lett. 2007 Sep 28;173(3):161-7. Epub 2007 Aug 2. PubMed PMID: 17826925.

7: Stray SJ, Zlotnick A. BAY 41-4109 has multiple effects on Hepatitis B virus capsid assembly. J Mol Recognit. 2006 Nov-Dec;19(6):542-8. PubMed PMID: 17006877.

8: Hallenberger S. Antiviral therapies. J Clin Virol. 2004 Apr;30 Suppl 1:S23-5. PubMed PMID: 15062765.

9: Deres K, Schröder CH, Paessens A, Goldmann S, Hacker HJ, Weber O, Krämer T, Niewöhner U, Pleiss U, Stoltefuss J, Graef E, Koletzki D, Masantschek RN, Reimann A, Jaeger R, Gross R, Beckermann B, Schlemmer KH, Haebich D, Rübsamen-Waigmann H. Inhibition of hepatitis B virus replication by drug-induced depletion of nucleocapsids. Science. 2003 Feb 7;299(5608):893-6. PubMed PMID: 12574631.

10: Weber O, Schlemmer KH, Hartmann E, Hagelschuer I, Paessens A, Graef E, Deres K, Goldmann S, Niewoehner U, Stoltefuss J, Haebich D, Ruebsamen-Waigmann H, Wohlfeil S. Inhibition of human hepatitis B virus (HBV) by a novel non-nucleosidic compound in a transgenic mouse model. Antiviral Res. 2002 May;54(2):69-78. PubMed PMID: 12062392.

Original: BML-284 HCl 853220-52-7, stock more than 100g

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: BML-284, also known as AMBMP and Wnt agonist 1, is a potent and selective activator of Wnt signaling. It enhances beta-catenin and increases transcript and protein levels of p-gp.

Name: BML-284 HCl 

CAS#: 853220-52-7 

Chemical Formula: C19H19ClN4O3 

Exact Mass: 

Molecular Weight: 386.84 

Elemental Analysis: C, 58.99; H, 4.95; Cl, 9.16; N, 14.48; O, 12.41

Synonym: AMBMP HCl; AMBMP Hydrochloride; BML284 HCl; Wnt Agonist; BML284 HCl; BML-284 HCl; BML 284 HCl;

IUPAC/Chemical Name: 4-N-(1,3-Benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine Hydrochloride

InChi Key: XZOFNDFDGVAIEH-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H18N4O3.ClH/c1-24-14-4-2-3-13(8-14)15-9-18(23-19(20)22-15)21-10-12-5-6-16-17(7-12)26-11-25-16;/h2-9H,10-11H2,1H3,(H3,20,21,22,23);1H

SMILES Code: NC1=NC(C2=CC=CC(OC)=C2)=CC(NCC3=CC=C(OCO4)C4=C3)=N1.[H]Cl

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: Tribulo P, Leão BCDS, Lehloenya KC, Mingoti GZ, Hansen PJ. Consequences of endogenous and exogenous WNT signaling for development of the preimplantation bovine embryo. Biol Reprod. 2017 Jun 1;96(6):1129-1141. doi: 10.1093/biolre/iox048. PubMed PMID: 28575156.

2: Narcisi R, Arikan OH, Lehmann J, Ten Berge D, van Osch GJ. Differential Effects of Small Molecule WNT Agonists on the Multilineage Differentiation Capacity of Human Mesenchymal Stem Cells. Tissue Eng Part A. 2016 Nov;22(21-22):1264-1273. Epub 2016 Oct 17. PubMed PMID: 27633010.

3: Fukuda Y, Sano O, Kazetani K, Yamamoto K, Iwata H, Matsui J. Tubulin is a molecular target of the Wnt-activating chemical probe. BMC Biochem. 2016 May 20;17(1):9. doi: 10.1186/s12858-016-0066-9. PubMed PMID: 27207629; PubMed Central PMCID: PMC4873989.

4: Wang H, Graves MW 2nd, Zhou H, Gu Z, Lamont RJ, Scott DA. 2-Amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine is an anti-inflammatory TLR-2, -4 and -5 response mediator in human monocytes. Inflamm Res. 2016 Jan;65(1):61-9. doi: 10.1007/s00011-015-0891-0. Epub 2015 Nov 27. PubMed PMID: 26613980; PubMed Central PMCID: PMC4703520.

5: Denicol AC, Dobbs KB, McLean KM, Carambula SF, Loureiro B, Hansen PJ. Canonical WNT signaling regulates development of bovine embryos to the blastocyst stage. Sci Rep. 2013;3:1266. doi: 10.1038/srep01266. Epub 2013 Feb 12. PubMed PMID: 23405280; PubMed Central PMCID: PMC3569626.

Original: Pifithrin-alpha 63208-82-2, stock more than 100g

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: Pifithrin-alpha is a p53 inactivator. It also has neuroprotective activity against strokes.

Name: Pifithrin-alpha 

CAS#: 63208-82-2 

Chemical Formula: C16H19BrN2OS 

Exact Mass: 366.0401 

Molecular Weight: 367.3 

Elemental Analysis: C, 52.32; H, 5.21; Br, 21.75; N, 7.63; O, 4.36; S, 8.73

Synonym: Pifithrin-alpha; Pifithrin alpha; PFT-alpha; PFTalpha; PFT alpha;

IUPAC/Chemical Name: 2-(2-Imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-methylphenyl)ethanone;hydrobromide

InChi Key: HAGVCKULCLQGRF-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H18N2OS.BrH/c1-11-6-8-12(9-7-11)14(19)10-18-13-4-2-3-5-15(13)20-16(18)17;/h6-9,17H,2-5,10H2,1H3;1H

SMILES Code: CC1=CC=C(C(CN2C(SC3=C2CCCC3)=N)=O)C=C1.[H]Br

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: Higgins SP, Tang Y, Higgins CE, Mian B, Zhang W, Czekay RP, Samarakoon R, Conti DJ, Higgins PJ. TGF-β1/p53 signaling in renal fibrogenesis. Cell Signal. 2017 Nov 28;43:1-10. doi: 10.1016/j.cellsig.2017.11.005. [Epub ahead of print] Review. PubMed PMID: 29191563.

2: Asjad HMM, Nasrollahi-Shirazi S, Sucic S, Freissmuth M, Nanoff C. Relax, Cool Down and Scaffold: How to Restore Surface Expression of Folding-Deficient Mutant GPCRs and SLC6 Transporters. Int J Mol Sci. 2017 Nov 14;18(11). pii: E2416. doi: 10.3390/ijms18112416. Review. PubMed PMID: 29135937; PubMed Central PMCID: PMC5713384.

3: Vávrová J, Rezáčová M. Importance of proapoptotic protein PUMA in cell radioresistance. Folia Biol (Praha). 2014;60(2):53-6. Review. PubMed PMID: 24785107.

4: Ding D, Allman BL, Salvi R. Review: ototoxic characteristics of platinum antitumor drugs. Anat Rec (Hoboken). 2012 Nov;295(11):1851-67. doi: 10.1002/ar.22577. Epub 2012 Oct 8. Review. PubMed PMID: 23044998.

5: Esposito E, Cuzzocrea S. New therapeutic strategy for Parkinson's and Alzheimer's disease. Curr Med Chem. 2010;17(25):2764-74. Review. PubMed PMID: 20586718.

6: Gudkov AV, Komarova EA. Dangerous habits of a security guard: the two faces of p53 as a drug target. Hum Mol Genet. 2007 Apr 15;16 Spec No 1:R67-72. Review. PubMed PMID: 17613549.

7: Bowen JM, Gibson RJ, Cummins AG, Keefe DM. Intestinal mucositis: the role of the Bcl-2 family, p53 and caspases in chemotherapy-induced damage. Support Care Cancer. 2006 Jul;14(7):713-31. Epub 2006 Feb 2. Review. PubMed PMID: 16453135.

8: Gudkov AV, Komarova EA. Prospective therapeutic applications of p53 inhibitors. Biochem Biophys Res Commun. 2005 Jun 10;331(3):726-36. Review. PubMed PMID: 15865929.

9: Dagher PC. Apoptosis in ischemic renal injury: roles of GTP depletion and p53. Kidney Int. 2004 Aug;66(2):506-9. Review. PubMed PMID: 15253698.

10: Howell SB. Resistance to apoptosis in prostate cancer cells. Mol Urol. 2000 Fall;4(3):225-9;discussion 231. Review. PubMed PMID: 11062378.

11: Komarova EA, Gudkov AV. Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry (Mosc). 2000 Jan;65(1):41-8. Review. PubMed PMID: 10702639.

Original:Pifithrin-beta HBr 511296-88-1, stock more than 100g

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: Pifithrin-beta, also known as QB102 and Cyclic-Pifithrin-α, is is p53 functional inhibitor. Pifithrin-β counteracts the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells.

Name: Pifithrin-beta HBr 

CAS#: 511296-88-1 (HBr) 

Chemical Formula: C16H17BrN2S 

Exact Mass: 

Molecular Weight: 349.29 

Elemental Analysis: C, 55.02; H, 4.91; Br, 22.88; N, 8.02; S, 9.18

Related CAS #: 60477-34-1 (free base)   511296-88-1 (HBr)   2109248-93-1 (HCl)    

Synonym: Pifithrin-β; Pifithrin-beta; PFTβ; PFT-β; QB102; QB102; QB102; Cyclic-Pifithrin-α

IUPAC/Chemical Name: 5,6,7,8-Tetrahydro-2-(4-methylphenyl)imidazo[2,1-b]benzothiazole hydrobromide

InChi Key: SGNCOAOESGSEOP-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H16N2S.BrH/c1-11-6-8-12(9-7-11)13-10-18-14-4-2-3-5-15(14)19-16(18)17-13;/h6-10H,2-5H2,1H3;1H

SMILES Code: CC1=CC=C(C2=CN3C(SC4=C3CCCC4)=N2)C=C1.[H]Br

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: Lisachev PD, Pustylnyak VO, Shtark MB. Sirt1 Regulates p53 Stability and Expression of Its Target S100B during Long-Term Potentiation in Rat Hippocampus. Bull Exp Biol Med. 2016 Feb;160(4):432-4. doi: 10.1007/s10517-016-3189-5. Epub 2016 Feb 23. PubMed PMID: 26902357.

2: Da Pozzo E, La Pietra V, Cosimelli B, Da Settimo F, Giacomelli C, Marinelli L, Martini C, Novellino E, Taliani S, Greco G. p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. ACS Chem Neurosci. 2014 May 21;5(5):390-9. doi: 10.1021/cn4002208. Epub 2014 Mar 28. PubMed PMID: 24646317; PubMed Central PMCID: PMC4030802.

3: Fernández-Cruz ML, Valdehita A, Alonso M, Mann E, Herradón B, Navas JM. Biological and chemical studies on aryl hydrocarbon receptor induction by the p53 inhibitor pifithrin-α and its condensation product pifithrin-β. Life Sci. 2011 Apr 25;88(17-18):774-83. doi: 10.1016/j.lfs.2011.02.019. Epub 2011 Feb 26. PubMed PMID: 21362431.

4: Christodoulou MS, Colombo F, Passarella D, Ieronimo G, Zuco V, De Cesare M, Zunino F. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg Med Chem. 2011 Mar 1;19(5):1649-57. doi: 10.1016/j.bmc.2011.01.039. Epub 2011 Jan 25. PubMed PMID: 21324703.

5: Waters FJ, Shavlakadze T, McIldowie MJ, Piggott MJ, Grounds MD. Use of pifithrin to inhibit p53-mediated signalling of TNF in dystrophic muscles of mdx mice. Mol Cell Biochem. 2010 Apr;337(1-2):119-31. doi: 10.1007/s11010-009-0291-2. Epub 2009 Oct 27. PubMed PMID: 19859789.

Original: A-804598 1125758-85-1, stock more than 100g

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Description: A-804598 is a P2X7 selective, competitive antagonist.

Name: A-804598 

CAS#: 1125758-85-1 

Chemical Formula: C19H17N5 

Exact Mass: 315.1484 

Molecular Weight: 315.38 

Elemental Analysis: C, 72.36; H, 5.43; N, 22.21

Synonym: A-804598; A 804598; A804598.

IUPAC/Chemical Name: N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine

InChi Key: PQYCRDPLPKGSME-AWEZNQCLSA-N

InChi Code: InChI=1S/C19H17N5/c1-14(15-7-3-2-4-8-15)23-19(22-13-20)24-18-11-5-10-17-16(18)9-6-12-21-17/h2-12,14H,1H3,(H2,22,23,24)/t14-/m0/s1

SMILES Code: C[C@H](/N=C(NC1=C2C=CC=NC2=CC=C1)/NC#N)C3=CC=CC=C3

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: Lord B, Ameriks MK, Wang Q, Fourgeaud L, Vliegen M, Verluyten W, Haspeslagh P, 

Carruthers NI, Lovenberg TW, Bonaventure P, Letavic MA, Bhattacharya A. A novel 

radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334. Eur J 

Pharmacol. 2015 Oct 15;765:551-9. doi: 10.1016/j.ejphar.2015.09.026. PubMed PMID: 

26386289.

2: Antonioli L, Giron MC, Colucci R, Pellegrini C, Sacco D, Caputi V, Orso G, 

Tuccori M, Scarpignato C, Blandizzi C, Fornai M. Involvement of the P2X7 

purinergic receptor in colonic motor dysfunction associated with bowel 

inflammation in rats. PLoS One. 2014 Dec 30;9(12):e116253. doi: 

10.1371/journal.pone.0116253. PubMed PMID: 25549098; PubMed Central PMCID: 

PMC4280204.

3: Catanzaro JM, Hueston CM, Deak MM, Deak T. The impact of the P2X7 receptor 

antagonist A-804598 on neuroimmune and behavioral consequences of stress. Behav 

Pharmacol. 2014 Sep;25(5-6):582-98. doi: 10.1097/FBP.0000000000000072. PubMed 

PMID: 25083574.

4: Able SL, Fish RL, Bye H, Booth L, Logan YR, Nathaniel C, Hayter P, Katugampola 

SD. Receptor localization, native tissue binding and ex vivo occupancy for 

centrally penetrant P2X7 antagonists in the rat. Br J Pharmacol. 2011 

Jan;162(2):405-14. doi: 10.1111/j.1476-5381.2010.01025.x. PubMed PMID: 20840537; 

PubMed Central PMCID: PMC3031061.

5: Donnelly-Roberts DL, Namovic MT, Surber B, Vaidyanathan SX, Perez-Medrano A, 

Wang Y, Carroll WA, Jarvis MF. [3H]A-804598 

([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, 

and selective antagonist radioligand for P2X7 receptors. Neuropharmacology. 2009 

Jan;56(1):223-9. doi: 10.1016/j.neuropharm.2008.06.012. PubMed PMID: 18602931.