BCAT-IN-2 是一种有效，具有选择性和口服活性的线粒体支链氨基转移酶 (BCATm) 抑制剂，pIC50 为 7.3。BCAT-IN-2 对 BCATm 显示出超过 BCATc 的选择性 (pIC50=6.6)。BCAT-IN-2 可用于肥胖和脂肪变性的研究。
BCAT-IN-2 is a potent, selective and orally active inhibitor of mitochondrial branched-chain aminotransferase (BCATm), with a pIC50 of 7.3. BCAT-IN-2 shows selectivity for BCATm over BCATc (pIC50=6.6). BCAT-IN-2 can be used for the research of obesity and dislipidema[1].
BCAT-IN-2 (compound 61) inhibits BCATm in differentiated primary human adipocyte, with pIC50 of 6.5[1].
BCAT-IN-2 (compound 61) (10-100 mg/kg; p.o.) increases the level of leucine from 473 μM to 1.2 mM at the dose of 100 mg/kg in mice[1].BCAT-IN-2 (5 mg/kg for p.o. and 1 mg/kg for i.v.) exhibits a high bioavailability (F=100%), long half-life (t1/2=9.2 h) and low clearance (Cl=0.3 mL/min/kg) in mice[1].
[1]. Bertrand SM, et, al. The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits. J Med Chem. 2015 Sep 24;58(18):7140-63.
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