1001094-46-7
1001094-46-7 structure
- Name: GS-9256
- Chemical Name: gs-9256
- CAS Number: 1001094-46-7
- Molecular Formula: C46H56ClF2N6O8PS
- Molecular Weight: 957.46100
- Catalog: Signaling Pathways Metabolic Enzyme/Protease HCV Protease
- Create Date: 2017-07-10 14:48:09
- Modify Date: 2024-01-28 17:35:22
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GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity[1].
| Name | gs-9256 |
|---|---|
| Synonyms |
gs9256
unii-8v42y78hru |
| Description | GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity[1]. |
|---|---|
| Related Catalog | |
| In Vitro | GS-9256 (0.002-0.183 μM) has a mean EC50 value of 20 nM in GT1b huh-luc cells with a replicon encoding luciferase[1]. GS-9256 (3 μM) retains wild-type activity against all NS5B and NS5A inhibitor-resistant mutations tested and is metabolically stable in microsomes and hepatocytes including rodents, dogs and humans[1]. |
| In Vivo | GS-9256 (1 mg/kg, i.v., 30 min) is highly bioavailable in mice (near 100%) and moderately bioavailable in rats (14%), dogs (21%) and monkeys (14%). The elimination half-life is approximately 2 hours in mice, 0.6 hours in rats, 5 hours in dogs, and 4 hours in monkeys[1]. The pharmacokinetic parameters of GS-9256(IV, 2 mg/kg mouse and 1 mg/kg rat, dog, monkey; Oral, 50 mg/kg mouse, 5 mg/kg rat and monkey, 4 mg/kg dog) - Parameters CD-1 mouse Sprague Dawley rat Beagle dog Cynomolgus monkey Intravenous CL(L/h/kg) 2.0 1.26 0.04 0.33 Vss (L/kg) 2.3 0.16 0.09 0.27 t1/2(h) 2.35 0.61 4.88 3.95 MRT(h) 1.15 0.13 2.11 0.82 Oral Tmax(h) 3.00 0.67 2.00 2.67 Cmax(nM) 11116 265 4369 604 t1/2(h) 1.31 0.53 4.22 4.42 AUC0-∞(nM*h) 58959 445 21043 2304 F(%) Complete 13.9 21 14 |
| Molecular Formula | C46H56ClF2N6O8PS |
|---|---|
| Molecular Weight | 957.46100 |
| Exact Mass | 956.32700 |
| PSA | 219.36000 |
| LogP | 10.28240 |