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PF-915275

Chemical Structure : PF-915275

CAS No.: 857290-04-1

PF-915275 (PF 915275;PF915275)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 350.3943
Formula C18H14N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

[1,1'-Biphenyl]-4-sulfonamide, N-(6-amino-2-pyridinyl)-4'-cyano-

References

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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