2581243-32-3

2581243-32-3 structure
2581243-32-3 structure
  • Name: BCAT-IN-1
  • Chemical Name: BCAT-IN-1
  • CAS Number: 2581243-32-3
  • Molecular Formula: C25H24BrN5O2S
  • Molecular Weight: 538.46
  • Catalog: Research Areas Metabolic Disease
  • Create Date: 2021-09-11 18:47:53
  • Modify Date: 2025-09-20 18:10:38
  • 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].

Name BCAT-IN-1
Description 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].
Related Catalog
Target

pIC50: 7.3 (BCATm)[1]

In Vitro 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].
In Vivo 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].
References

[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.

Molecular Formula C25H24BrN5O2S
Molecular Weight 538.46
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