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 (3)
Reviews
Literature (1)

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

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

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.

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

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 the degree 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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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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Literature in this Area

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