GSK973

Name: GSK973
Brand: TargetMol
SKU: T39601
Rating: 4.5 (1 reviews)

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产品编号 T39601Cas号 2138473-38-6

别名 GSK973

GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5.

GSK973

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产品编号 T39601 别名 GSK973Cas号 2138473-38-6

规格	价格	库存	数量
25 mg	¥ 10,600	6-8周

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产品介绍

生物活性

产品描述	GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5.
体内活性	GSK973 (1 mg/kg; i.v.) treatment shows the CL, CI renal , V ss , and T 1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively[1]. GSK973 (3 mg/kg; p.o) treatment shows the F po of 48%[1]. Animal Model: Male Wistar Han Rats[1]Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: I.v. Result: The CL, CI renal , V ss , and T 1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.
别名	GSK973