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住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian
QQ: 2393923585
Description: Apabetalone, also known as RVX-208, is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. RVX-208 may be a promising new approach to the treatment of atherosclerosis.
Name: Apabetalone
CAS#: 1044870-39-4
Chemical Formula: C20H22N2O5
Exact Mass: 370.15287
Molecular Weight: 370.39908
Elemental Analysis: C, 64.85; H, 5.99; N, 7.56; O, 21.60
Purity: >98% (or refer to the Certificate of Analysis)
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).
REFERENCES
1: Barylski M, Toth PP, Nikolic D, Banach M, Rizzo M, Montalto G. Emerging therapies for raising high-density lipoprotein cholesterol (HDL-C) and augmenting HDL particle functionality. Best Pract Res Clin Endocrinol Metab. 2014 Jun;28(3):453-61. doi: 10.1016/j.beem.2013.11.001. Epub 2013 Nov 15. PubMed PMID: 24840270.
2: McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E, Suto RK, Wong NC, Wagner GS, Hansen HC, Young PR. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PubMed PMID: 24391744; PubMed Central PMCID: PMC3877016.
3: Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PubMed PMID: 24248379; PubMed Central PMCID: PMC3856850.
5: Khmelnitsky YL, Mozhaev VV, Cotterill IC, Michels PC, Boudjabi S, Khlebnikov V, Madhava Reddy M, Wagner GS, Hansen HC. In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208). Eur J Med Chem. 2013 Jun;64:121-8. doi: 10.1016/j.ejmech.2013.03.062. Epub 2013 Apr 10. PubMed PMID: 23644195.
6: Joy TR. Novel HDL-based therapeutic agents. Pharmacol Ther. 2012 Jul;135(1):18-30. doi: 10.1016/j.pharmthera.2012.03.004. Epub 2012 Mar 23. Review. PubMed PMID: 22465158.
7: Nicholls SJ, Gordon A, Johannson J, Ballantyne CM, Barter PJ, Brewer HB, Kastelein JJ, Wong NC, Borgman MR, Nissen SE. ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies. Cardiovasc Drugs Ther. 2012 Apr;26(2):181-7. doi: 10.1007/s10557-012-6373-5. PubMed PMID: 22349989.
8: Rvx 208. Drugs R D. 2011;11(2):207-13. doi: 10.2165/11595140-000000000-00000. Review. PubMed PMID: 21679009; PubMed Central PMCID: PMC3585949.
9: Shah PK. Atherosclerosis: targeting endogenous apo A-I--a new approach for raising HDL. Nat Rev Cardiol. 2011 Apr;8(4):187-8. doi: 10.1038/nrcardio.2011.37. Epub 2011 Mar 1. PubMed PMID: 21364534.
10: Horowitz JD, Rosenson RS, McMurray JJ, Marx N, Remme WJ. Clinical Trials Update AHA Congress 2010. Cardiovasc Drugs Ther. 2011 Feb;25(1):69-76. doi: 10.1007/s10557-011-6285-9. PubMed PMID: 21340529.
11: Nicholls SJ, Gordon A, Johansson J, Wolski K, Ballantyne CM, Kastelein JJ, Taylor A, Borgman M, Nissen SE. Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial. J Am Coll Cardiol. 2011 Mar 1;57(9):1111-9. doi: 10.1016/j.jacc.2010.11.015. Epub 2011 Jan 20. PubMed PMID: 21255957.
12: Davidson MH. Apolipoprotein A-I therapy promise, challenges, and disappointment. J Am Coll Cardiol. 2011 Mar 1;57(9):1120-1. doi: 10.1016/j.jacc.2010.11.025. Epub 2011 Jan 20. PubMed PMID: 21255956.
13: Inazu A. [Novel therapy for atherosclerosis and inflammatory vascular disease]. Nihon Rinsho. 2011 Jan;69(1):105-9. Review. Japanese. PubMed PMID: 21226269.
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian
QQ: 2393923585
Description: Apabetalone, also known as RVX-208, is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. RVX-208 may be a promising new approach to the treatment of atherosclerosis.
Name: Apabetalone
CAS#: 1044870-39-4
Chemical Formula: C20H22N2O5
Exact Mass: 370.15287
Molecular Weight: 370.39908
Elemental Analysis: C, 64.85; H, 5.99; N, 7.56; O, 21.60
Purity: >98% (or refer to the Certificate of Analysis)
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).
REFERENCES
1: Barylski M, Toth PP, Nikolic D, Banach M, Rizzo M, Montalto G. Emerging therapies for raising high-density lipoprotein cholesterol (HDL-C) and augmenting HDL particle functionality. Best Pract Res Clin Endocrinol Metab. 2014 Jun;28(3):453-61. doi: 10.1016/j.beem.2013.11.001. Epub 2013 Nov 15. PubMed PMID: 24840270.
2: McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E, Suto RK, Wong NC, Wagner GS, Hansen HC, Young PR. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PubMed PMID: 24391744; PubMed Central PMCID: PMC3877016.
3: Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PubMed PMID: 24248379; PubMed Central PMCID: PMC3856850.
5: Khmelnitsky YL, Mozhaev VV, Cotterill IC, Michels PC, Boudjabi S, Khlebnikov V, Madhava Reddy M, Wagner GS, Hansen HC. In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208). Eur J Med Chem. 2013 Jun;64:121-8. doi: 10.1016/j.ejmech.2013.03.062. Epub 2013 Apr 10. PubMed PMID: 23644195.
6: Joy TR. Novel HDL-based therapeutic agents. Pharmacol Ther. 2012 Jul;135(1):18-30. doi: 10.1016/j.pharmthera.2012.03.004. Epub 2012 Mar 23. Review. PubMed PMID: 22465158.
7: Nicholls SJ, Gordon A, Johannson J, Ballantyne CM, Barter PJ, Brewer HB, Kastelein JJ, Wong NC, Borgman MR, Nissen SE. ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies. Cardiovasc Drugs Ther. 2012 Apr;26(2):181-7. doi: 10.1007/s10557-012-6373-5. PubMed PMID: 22349989.
8: Rvx 208. Drugs R D. 2011;11(2):207-13. doi: 10.2165/11595140-000000000-00000. Review. PubMed PMID: 21679009; PubMed Central PMCID: PMC3585949.
9: Shah PK. Atherosclerosis: targeting endogenous apo A-I--a new approach for raising HDL. Nat Rev Cardiol. 2011 Apr;8(4):187-8. doi: 10.1038/nrcardio.2011.37. Epub 2011 Mar 1. PubMed PMID: 21364534.
10: Horowitz JD, Rosenson RS, McMurray JJ, Marx N, Remme WJ. Clinical Trials Update AHA Congress 2010. Cardiovasc Drugs Ther. 2011 Feb;25(1):69-76. doi: 10.1007/s10557-011-6285-9. PubMed PMID: 21340529.
11: Nicholls SJ, Gordon A, Johansson J, Wolski K, Ballantyne CM, Kastelein JJ, Taylor A, Borgman M, Nissen SE. Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial. J Am Coll Cardiol. 2011 Mar 1;57(9):1111-9. doi: 10.1016/j.jacc.2010.11.015. Epub 2011 Jan 20. PubMed PMID: 21255957.
12: Davidson MH. Apolipoprotein A-I therapy promise, challenges, and disappointment. J Am Coll Cardiol. 2011 Mar 1;57(9):1120-1. doi: 10.1016/j.jacc.2010.11.025. Epub 2011 Jan 20. PubMed PMID: 21255956.
13: Inazu A. [Novel therapy for atherosclerosis and inflammatory vascular disease]. Nihon Rinsho. 2011 Jan;69(1):105-9. Review. Japanese. PubMed PMID: 21226269.
14: Bailey D, Jahagirdar R, Gordon A, Hafiane A, Campbell S, Chatur S, Wagner GS, Hansen HC, Chiacchia FS, Johansson J, Krimbou L, Wong NC, Genest J. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9. doi: 10.1016/j.jacc.2010.02.035. Erratum in: J Am Coll Cardiol. 2010 Aug 31;56(10):825. PubMed PMID: 20513599.
15: McNeill E. RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases. Curr Opin Investig Drugs. 2010 Mar;11(3):357-64. Review. PubMed PMID: 20178050.
16: Wong NC. Coronary Artery Disease - Eighth International Congress. From prevention to intervention. IDrugs. 2009 Dec;12(12):742-6. PubMed PMID: 19943213
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian
QQ: 2393923585
Description: Ivacaftor, also known as VX-770, is a drug used to treat cystic fibrosis in people with certain mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene, who account for 4–5% cases of cystic fibrosis, and is included in a combination drug, lumacaftor/ivacaftor, which is used to treat people with cystic fibrosis who have the F508del mutation in CFTR. Ivacaftor is a "potentiator" of CFTR, meaning it increases the probability that the defective channel will be open and allow chloride ions pass through the channel pore.
Name: Ivacaftor
CAS#: 873054-44-5
Chemical Formula: C24H28N2O3
Exact Mass: 392.20999
Molecular Weight: 392.49072
Elemental Analysis: C, 73.44; H, 7.19; N, 7.14; O, 12.23
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: >5 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: Davis PB. Therapy for cystic fibrosis--the end of the beginning? N Engl J Med. 2011 Nov 3;365(18):1734-5. PubMed PMID: 22047565.
2: Ramsey BW, Davies J, McElvaney NG, Tullis E, Bell SC, DřevÃnek P, Griese M, McKone EF, Wainwright CE, Konstan MW, Moss R, Ratjen F, Sermet-Gaudelus I, Rowe SM, Dong Q, Rodriguez S, Yen K, Ordoñez C, Elborn JS; VX08-770-102 Study Group. A CFTR potentiator in patients with cystic fibrosis and the G551D mutation. N Engl J Med. 2011 Nov 3;365(18):1663-72. PubMed PMID: 22047557; PubMed Central PMCID: PMC3230303.
3: Kim Chiaw P, Eckford PD, Bear CE. Insights into the mechanisms underlying CFTR channel activity, the molecular basis for cystic fibrosis and strategies for therapy. Essays Biochem. 2011 Sep 7;50(1):233-48. PubMed PMID: 21967060.
4: Pyle LC, Ehrhardt A, Mitchell LH, Fan L, Ren A, Naren AP, Li Y, Clancy JP, Bolger GB, Sorscher EJ, Rowe SM. Regulatory domain phosphorylation to distinguish the mechanistic basis underlying acute CFTR modulators. Am J Physiol Lung Cell Mol Physiol. 2011 Oct;301(4):L587-97. Epub 2011 Jul 1. PubMed PMID: 21724857; PubMed Central PMCID: PMC3191754.
5: Opar A. Excitement mounts for first disease-modifying cystic fibrosis drugs. Nat Rev Drug Discov. 2011 Jul 1;10(7):479-80. doi: 10.1038/nrd3488. PubMed PMID: 21720393.
6: Sheridan C. First cystic fibrosis drug advances towards approval. Nat Biotechnol. 2011 Jun 7;29(6):465-6. doi: 10.1038/nbt0611-465. PubMed PMID: 21654649.
7: Yu W, Chiaw PK, Bear CE. Probing conformational rescue induced by a chemical corrector of F508del-cystic fibrosis transmembrane conductance regulator (CFTR) mutant. J Biol Chem. 2011 Jul 15;286(28):24714-25. Epub 2011 May 21. PubMed PMID: 21602569; PubMed Central PMCID: PMC3137047.
9: Dolgin E. Mutation-specific cystic fibrosis treatments on verge of approval. Nat Med. 2011 Apr;17(4):396-7. PubMed PMID: 21475213.
10: Erlinger S. Molecular repair of a defective CFTR protein in cystic fibrosis. Clin Res Hepatol Gastroenterol. 2011 Apr;35(4):254-6. Epub 2011 Feb 23. PubMed PMID: 21349786.
11: Antoniu SA. Cystic fibrosis transmembrane regulator potentiators as promising cystic fibrosis therapies. Expert Opin Investig Drugs. 2011 Mar;20(3):423-5. Epub 2011 Feb 9. PubMed PMID: 21303308.
12: Welsh MJ. Targeting the basic defect in cystic fibrosis. N Engl J Med. 2010 Nov 18;363(21):2056-7. PubMed PMID: 21083391.
13: Accurso FJ, Rowe SM, Clancy JP, Boyle MP, Dunitz JM, Durie PR, Sagel SD, Hornick DB, Konstan MW, Donaldson SH, Moss RB, Pilewski JM, Rubenstein RC, Uluer AZ, Aitken ML, Freedman SD, Rose LM, Mayer-Hamblett N, Dong Q, Zha J, Stone AJ, Olson ER, Ordoñez CL, Campbell PW, Ashlock MA, Ramsey BW. Effect of VX-770 in persons with cystic fibrosis and the G551D-CFTR mutation. N Engl J Med. 2010 Nov 18;363(21):1991-2003. PubMed PMID: 21083385; PubMed Central PMCID: PMC3148255.
14: Sloane PA, Rowe SM. Cystic fibrosis transmembrane conductance regulator protein repair as a therapeutic strategy in cystic fibrosis. Curr Opin Pulm Med. 2010 Nov;16(6):591-7. Review. PubMed PMID: 20829696.
15: Van Goor F, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A, Zhou J, McCartney J, Arumugam V, Decker C, Yang J, Young C, Olson ER, Wine JJ, Frizzell RA, Ashlock M, Negulescu P. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30. Epub 2009 Oct 21. PubMed PMID: 19846789; PubMed Central PMCID: PMC2773991.
16: Jones AM, Helm JM. Emerging treatments in cystic fibrosis. Drugs. 2009 Oct 1;69(14):1903-10. doi: 10.2165/11318500-000000000-00000. PubMed PMID: 19747007.
