Name | N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide |
Synonyms | PF915275 PF 915275 PF-915275 N-(6-aminopyridin-2-yl)-4-(4-cyanophenyl)benzenesulfonamide N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide [1,1'-Biphenyl]-4-sulfonamide, N-(6-amino-2-pyridinyl)-4'-cyano- |
CAS | 857290-04-1 |
Molecular Formula | C18H14N4O2S |
Molar Mass | 350.39 |
Density | 1.44±0.1 g/cm3(Predicted) |
Boling Point | 610.9±65.0 °C(Predicted) |
pKa | 7.97±0.29(Predicted) |
Storage Condition | Store at RT |
Use | PF-915275 is a potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 2.3 nM) PF-915275 inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC50 = 15 nM) and has antidiabetic activity in vivo. |
Reference Show more | 1: Zhao L, Pan Y, Peng K, Wang Z, Li J, Li D, Tong C, Wang Y, Liang G. Inhibition of 11β-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice. J Mol Endocrinol. 2015 Oct;55(2):119-31. doi: 10.1530/JME-14-0268. Epub 2015 Jul 28. PubMed PMID: 26220348. 2: Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24. PubMed PMID: 23489629. 3: Dorniak P, Welsh TH Jr, Bazer FW, Spencer TE. Cortisol and interferon tau regulation of endometrial function and conceptus development in female sheep. Endocrinology. 2013 Feb;154(2):931-41. doi: 10.1210/en.2012-1909. Epub 2012 Dec 21. PubMed PMID: 23264615. 4: Lee SE, Kim JM, Jeong MK, Zouboulis CC, Lee SH. 11β-hydroxysteroid dehydrogenase type 1 is expressed in human sebaceous glands and regulates glucocorticoid-induced lipid synthesis and toll-like receptor 2 expression in SZ95 sebocytes. Br J Dermatol. 2013 Jan;168(1):47-55. doi: 10.1111/bjd.12009. PubMed PMID: 22897663. 5: Harno E, White A. Will treating diabetes with 11β-HSD1 inhibitors affect the HPA axis? Trends Endocrinol Metab. 2010 Oct;21(10):619-27. doi: 10.1016/j.tem.2010.06.00 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.854 ml | 14.27 ml | 28.54 ml |
5 mM | 0.571 ml | 2.854 ml | 5.708 ml |
10 mM | 0.285 ml | 1.427 ml | 2.854 ml |
5 mM | 0.057 ml | 0.285 ml | 0.571 ml |