| Bioactivity | 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]. | ||||||||||||
| Target | pIC50: 7.3 (BCATm), 6.6 (BCATc) | ||||||||||||
| Invitro | BCAT-IN-2 (compound 61) inhibits BCATm in differentiated primary human adipocyte, with pIC50 of 6.5[1]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | BCAT-IN-2 | ||||||||||||
| CAS | 1800024-45-6 | ||||||||||||
| Formula | C17H14ClF2N5O | ||||||||||||
| Molar Mass | 377.78 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
BCAT-IN-2
CAS: 1800024-45-6 F: C17H14ClF2N5O W: 377.78
BCAT-IN-2 is a potent, selective and orally active inhibitor of mitochondrial branched-chain aminotransferase (BCATm), w
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