857290-04-1

857290-04-1 structure

Name: PF 915275
Chemical Name: N-(6-aminopyridin-2-yl)-4-(4-cyanophenyl)benzenesulfonamide
CAS Number: 857290-04-1
Molecular Formula: C₁₈H₁₄N₄O₂S
Molecular Weight: 350.394
Catalog: Research Areas Metabolic Disease
Create Date: 2017-11-17 12:00:41
Modify Date: 2024-01-15 13:10:09
PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

Name	N-(6-aminopyridin-2-yl)-4-(4-cyanophenyl)benzenesulfonamide
Synonyms	N-(6-Amino-2-pyridinyl)-4'-cyano-4-biphenylsulfonamide [1,1'-Biphenyl]-4-sulfonamide, N-(6-amino-2-pyridinyl)-4'-cyano- 4'-cyanobiphenyl-4-sulfonic acid (6-aminopyridin-2-yl)amide N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide PF-915275

Description	PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Metabolic Disease
References	[1]. Bhat BG, et al. 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 11 -hydroxysteroid dehydrogenase type 1, in cynomolg [2]. Siu M, et al. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7.

Density	1.4±0.1 g/cm3
Boiling Point	610.9±65.0 °C at 760 mmHg
Molecular Formula	C₁₈H₁₄N₄O₂S
Molecular Weight	350.394
Flash Point	323.3±34.3 °C
Exact Mass	350.083740
PSA	117.25000
LogP	2.06
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.709
Storage condition	2-8℃

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