Chemical Structure : PF-915275
CAS No.: 857290-04-1
Catalog No.: PC-45408Not For Human Use, Lab Use Only.
PF-915275 is a specific and potent inhibitor of the human11β-HSD1 with Ki of 2.3 nM and in vitro HEK293 EC50 of 15 nM, with minimal inhibitory activity toward the mouse enzyme (Ki=750 nM).
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PF-915275 is a specific and potent inhibitor of the human11β-HSD1 with Ki of 2.3 nM and in vitro HEK293 EC50 of 15 nM, with minimal inhibitory activity toward the mouse enzyme (Ki=750 nM).
PF-915275 does not significantly inhibit 11β-HSD2.
PF-915275 dose-dependently inhibits 11betaHSD1-mediated conversion of prednisone to prednisolone (3-mg/kg, 87% inhibition) in cynomolgus monkeys.
M.Wt | 350.3943 | |
Formula | C18H14N4O2S | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: ≥ 31 mg/mL |
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Chemical Name/SMILES |
[1,1'-Biphenyl]-4-sulfonamide, N-(6-amino-2-pyridinyl)-4'-cyano- |
1. Siu M, et al. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7.
2. Bhat BG, et al. J Pharmacol Exp Ther. 2008 Jan;324(1):299-305.
3. Dorniak P, et al. Endocrinology. 2013 Feb;154(2):931-41.
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