GS-9256

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GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity.

For research use only. We do not sell to patients.

GS-9256 Chemical Structure

CAS No. : 1001094-46-7

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Description

GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
	t_1/2(h)	2.35	0.61	4.88	3.95
	MRT(h)	1.15	0.13	2.11	0.82
Oral	T_max(h)	3.00	0.67	2.00	2.67
	C_max(nM)	11116	265	4369	604
	t_1/2(h)	1.31	0.53	4.22	4.42
	AUC_0-∞(nM*h)	58959	445	21043	2304
	F(%)	Complete	13.9	21	14

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

957.46

Formula

C₄₆H₅₆ClF₂N₆O₈PS

CAS No.

1001094-46-7

Unlabeled CAS

SMILES

O=C(OC1CCCC1)N[C@H]2CCCCCCC[C@@]3([H])[C@](C3)(P(O)(CC4=C(F)C=CC=C4F)=O)NC([C@@](C[C@@H](OC5=CC(C6=CSC(NC(C)C)=N6)=NC7=C(Cl)C(OC)=CC=C57)C8)([H])N8C2=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Huiling Yang, et al. Preclinical characterization of the novel HCV NS3 protease inhibitor GS-9256. Antivir Ther. 2017;22(5):413-420. [Content Brief]

GS-9256 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GS-92561001094-46-7GS9256GS 9256HCV ProteaseHCV NS3proteaseantiviralInhibitorinhibitorinhibit

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