GS-9901

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GS-9901

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1640247-87-5

GS-9901 是高度选择性的、口服有效的PI3Kδ的抑制剂，其IC₅₀值为 1 nM。有用于风湿性关节炎的潜能。

生物活性

GS-9901 is a highly selective and orally activePI3Kδinhibitor, with anIC₅₀of 1 nM. Has potential to treat rheumatoid arthritis^[1].

IC₅₀& Target

PI3Kδ

1 nM (IC₅₀)

体内研究
(In Vivo)

GS-9901 (0.3/1/3 mg/kg, orally, twice daily for 7 days) demonstrates efficacy in a rat model of arthritis and is predicted to be suitable for q.d. dosing in humans^[1].

Animal Model:	Female Lewis rats with established collagen-induced arthritis (CIA)^[1].
Dosage:	0.3 mg/kg, 1 mg/kg, and 3 mg/kg.
Administration:	Orally, twice-daily for 7 days starting on the 10th day after the second collagen immunization.
Result:	Demonstrated significant reduction in ankle swelling in rats treated with 0.3 mg/kg 35 (31% reduction), 1 mg/kg 35 (67%), and 3 mg/kg 35 (65%). Plasma concentrations measured on day 7 (12 h after last dose) were consistent with maintaining approximately 60%, 80%, and >90% inhibition of PI3Kδ at 0.3, 1.0, and 3 mg/kg doses, respectively, at trough levels.

Clinical Trial

分子量

477.88

Formula

C₂₂H₁₇ClFN₉O

CAS 号

1640247-87-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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