产品
编 号：F741690
分子式：C22H14ClF3N2O3
分子量：446.81
分子式：C22H14ClF3N2O3
分子量：446.81
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: 2639638-66-5
产品详情
生物活性：
BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer.
体内研究：
BAY-069 exhibits high metabolic stability after incubation with human liver microsomes (CLblood = 0.11 L/h/kg) and moderate metabolic stability after incubation with rat hepatocytes (CLblood = 1.8 L/h/kg); shows high permeability through Caco-2 cell monolayers with no hint of efflux.BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2).Animal Model:Male Wistar rats
Dosage:0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.
Administration:i.v. or p.o.; single dosage
Result:Pharmacokinetic Parameters of BAY-069 in male Wistar rats.CLblood (L/h/kg)Vss (L/kg) t1/2 (h), i.v. AUCnorm (kg·h/L), i.v. AUCnorm (kg·h/L), p.o. F (%), p.o.
0.640.251.62.92.589
体外研究：
BAY-069 (compound 36a) (70 nM-50 μM; 72 h) inhibits cell proliferation of U-87 and MDA-MB-231.
BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer.
体内研究：
BAY-069 exhibits high metabolic stability after incubation with human liver microsomes (CLblood = 0.11 L/h/kg) and moderate metabolic stability after incubation with rat hepatocytes (CLblood = 1.8 L/h/kg); shows high permeability through Caco-2 cell monolayers with no hint of efflux.BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2).Animal Model:Male Wistar rats
Dosage:0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.
Administration:i.v. or p.o.; single dosage
Result:Pharmacokinetic Parameters of BAY-069 in male Wistar rats.CLblood (L/h/kg)Vss (L/kg) t1/2 (h), i.v. AUCnorm (kg·h/L), i.v. AUCnorm (kg·h/L), p.o. F (%), p.o.
0.640.251.62.92.589
体外研究：
BAY-069 (compound 36a) (70 nM-50 μM; 72 h) inhibits cell proliferation of U-87 and MDA-MB-231.
产品资料
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