PF 915275
Tocris Bioscience, part of Bio-Techne | Catalog # 3291
Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor
Key Product Details
Description
Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor
Product Description
PF 915275 is a 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.Product Specifications
Molecular Weight
350.39
Formula
C18H14N4O2S
Storage
Store at RT
Purity
≥98% (HPLC)
Chemical Name
N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
CAS Number
857290-04-1
PubChem ID
23725123
InChI Key
ZESFDAKNYJQYKO-UHFFFAOYSA-N
SMILES
NC1=NC(NS(C(C=C3)=CC=C3C2=CC=C(C#N)C=C2)(=O)=O)=CC=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.04 | 100 |
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the 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 Specific Notices for PF 915275
For research use only
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