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BCAT-IN-1
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。
BCAT-IN-1图片
CAS NO:1875078-61-7
包装与价格：
包装价格(元)
5mg电议
10mg电议

产品介绍
BCAT-IN-1 是一种有效，选择性和具有口服活性的 BCATm 抑制剂，pIC50 值为 7.3。BCAT-IN-1 对 BCATm 的选择性比 BCATc 高 100 倍 (pIC50=5.4)。BCAT-IN-1 可用于代谢疾病的研究。
Cas No.1875078-61-7
分子式C25H24BrN5O2S
分子量538.46
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BCAT-IN-1 is a potent, selective and orally active inhibitor of BCATm, with a pIC50 of 7.3. BCAT-IN-1 shows 100-fold selectivity for BCATm over BCATc (pIC50=5.4). BCAT-IN-1 can be used for the research of metabolic diseases[1].

BCAT-IN-1 (compound 8b) inhibits BCATm in human cells, with a pIC50 of 7.0[1].BCAT-IN-1 inhibits mouse BCATm, with pIC50 of 5.9 in the cellular assay[1].

BCAT-IN-1 (compound 8b) (30-300 mg/kg; p.o.) increases the level of c BCAAs in an acute mouse model over an extended duration[1].BCAT-IN-1 (5 mg/kg; p.o.) exhibits oral bioavailability (F=28%) and Cmax (1648 ng/mL) in mice[1].BCAT-IN-1 (1 mg/kg; i.v.) exhibits half-life (t1/2=9.2 h) and clearance (Cl=4.0 mL/min/kg) in mice[1].

[1]. Deng H, et, al. Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors. ACS Med Chem Lett. 2016 Feb 8;7(4):379-84.