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。
货号:ajcx37028
CAS:1875078-61-7
分子式:C25H24BrN5O2S
分子量：538.46
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.