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
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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] |
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| Related Catalog | |
| References |
| 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℃ |