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857290-04-1

857290-04-1 structure
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
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℃