产品
编 号：F001092
分子式：C46H56ClF2N6O8PS
分子量：957.46
分子式：C46H56ClF2N6O8PS
分子量：957.46
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CAS No: 1001094-46-7
产品详情
生物活性：
GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity.
体内研究：
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. 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) -ParametersCD-1 mouseSprague Dawley ratBeagle dogCynomolgus monkeyIntravenousCL(L/h/kg)2.01.260.040.33
Vss (L/kg)2.30.160.090.27
t1/2(h)2.350.614.883.95
MRT(h)1.150.132.110.82
OralTmax(h)3.000.672.002.67
Cmax(nM)111162654369604
t1/2(h)1.310.534.224.42
AUC0-∞(nM*h)58959445210432304
F(%)Complete13.92114
体外研究：
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. 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.
GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity.
体内研究：
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. 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) -ParametersCD-1 mouseSprague Dawley ratBeagle dogCynomolgus monkeyIntravenousCL(L/h/kg)2.01.260.040.33
Vss (L/kg)2.30.160.090.27
t1/2(h)2.350.614.883.95
MRT(h)1.150.132.110.82
OralTmax(h)3.000.672.002.67
Cmax(nM)111162654369604
t1/2(h)1.310.534.224.42
AUC0-∞(nM*h)58959445210432304
F(%)Complete13.92114
体外研究：
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. 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.
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