产品
编 号：F749286
分子式：C23H23FN2O4
分子量：410.44
分子式：C23H23FN2O4
分子量：410.44
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2138473-38-6
产品详情
生物活性：
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
体内研究：
GSK973 (1 mg/kg; i.v.) treatment shows the CL, CIrenal, Vss, and T1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%.Animal Model:Male Wistar Han Rats
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:I.v.
Result:The CL, CIrenal, Vss, and T1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
体内研究：
GSK973 (1 mg/kg; i.v.) treatment shows the CL, CIrenal, Vss, and T1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%.Animal Model:Male Wistar Han Rats
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:I.v.
Result:The CL, CIrenal, Vss, and T1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.
产品资料
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