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Potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 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.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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 will affect the solvent volumes required to prepare stock solutions.
|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|
References are publications that support the biological activity of the product.
Bhat et al (2008) 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. 324 299 PMID: 17921190
Fotsch and Wang (2008) 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. 51 4851 PMID: 18652443
Courtney et al (2008) Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 93 550 PMID: 17986636
If you know of a relevant reference for PF 915275, please let us know.
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Keywords: PF 915275, PF 915275 supplier, Potent, selective, 11β-hydroxysteroid, beta-hydroxysteroid, dehydrogenases, type, 1, 11βHSD1, 11betaHSD1, inhibitors, inhibits, PF915275, 11b-Hydroxysteroid, Dehydrogenase, 3291, Tocris Bioscience
3 Citations for PF 915275
Citations are publications that use Tocris products. Selected citations for PF 915275 include:
Youm et al (2013) Local blockade of glucocorticoid activation reverses stress- and glucocorticoid-induced delays in cutaneous wound healing. Wound Repair Regen 21 715 PMID: 23927023
Matsumura et al (2018) Local cortisol activation is involved in EGF-induced immunosuppression. Dermatoendocrinol 9 e1412018 PMID: 29484105
Chang (2018) An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells. BMC Pharmacol Toxicol 19 45 PMID: 30021644
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