PF 915275

Name: PF 915275
Brand: Tocris Bioscience
SKU: 3291

Tocris Bioscience, part of Bio-Techne | Catalog # 3291

Citations (8)

COA / SDS

Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor

Key Product Details

Description:	Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor
Chemical Name:	N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	350.39

View Full Technical Details for PF 915275

Technical Data
Citations

Biological Activity for PF 915275

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.

Compound Libraries for PF 915275

PF 915275 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PF 915275

M. Wt	350.39
Formula	C₁₈H₁₄N₄O₂S
Storage	Store at RT
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 915275

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 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

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References for PF 915275

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