PF 915275

Key Product Details

Product Description

PF 915275 is a potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (K_i = 2.3 nM) that displays little activity at 11βHSD2 (1.5% inhibition at 10 μM). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC₅₀ = 15 nM) and has antidiabetic activity in vivo. Orally active.

Product Specifications for PF 915275

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PF 915275

The following data is based on the product molecular weight 350.39.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.85 mL	14.27 mL	28.54 mL
5 mM	0.57 mL	2.85 mL	5.71 mL
10 mM	0.29 mL	1.43 mL	2.85 mL
50 mM	0.06 mL	0.29 mL	0.57 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 7 publications citing the usage of this product.

• Fotsch and Wang Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J.Med.Chem. 2008 PMID: 18652443
• Courtney Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 2008 PMID: 17986636
• Bhat Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 in cynomolgus monke J.Pharmacol.Exp.Ther. 2008 PMID: 17921190

Product Documents for PF 915275