PF 915275

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Cat.No. 3291 - PF 915275 | C18H14N4O2S | CAS No. 857290-04-1
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)
Datasheet
Citations
Literature

Biological Activity

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.

Compound Libraries

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.04 100

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.

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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Keywords: Potent selective 11β-hydroxysteroid beta-hydroxysteroid dehydrogenases type 1 11βHSD1 11betaHSD1 inhibitors inhibits PF915275 11b-Hydroxysteroid Dehydrogenase

Citations for PF 915275

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