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.
All Tocris products are intended for laboratory research use only.
|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 solvent 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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
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.
View Related Products by Product Action
Keywords: Potent selective 11β-hydroxysteroid beta-hydroxysteroid dehydrogenases type 1 11βHSD1 11betaHSD1 inhibitors inhibits PF915275 11b-Hydroxysteroid Dehydrogenase
Citations for PF 915275
Citations are publications that use Tocris products.
Currently there are no citations for PF 915275. Do you know of a great paper that uses PF 915275 from Tocris? If so please let us know.
Literature in this Area
New Product Guide (Spring/Summer 2017)New
Our new product guide highlights over 130 new products added to the Tocris Bioscience range during the first half of 2017.
- 7-TM Receptors
- Enzyme-Linked Receptors
- Ion Channels
- Nuclear Receptors
- Cell Metabolism
- Fluorescent Imaging
- Signal Transduction
- Stem Cells