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BCAT-IN-2

Names

[ CAS No. ]:
1800024-45-6

[ Name ]:
BCAT-IN-2

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[Target]

pIC50: 7.3 (BCATm), 6.6 (BCATc)[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H14ClF2N5O

[ Molecular Weight ]:
377.78

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xi


Related Compounds