Bioactivity | GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity[1]. |
Invitro | 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) - |
Name | GS-9256 |
CAS | 1001094-46-7 |
Formula | C46H56ClF2N6O8PS |
Molar Mass | 957.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Huiling Yang, et al. Preclinical characterization of the novel HCV NS3 protease inhibitor GS-9256. Antivir Ther. 2017;22(5):413-420. |