BCATc Inhibitor 2

Modify Date: 2024-01-04 12:09:29

BCATc Inhibitor 2 Structure
BCATc Inhibitor 2 structure
Common Name BCATc Inhibitor 2
CAS Number 406191-34-2 Molecular Weight 418.77
Density N/A Boiling Point N/A
Molecular Formula C16H10ClF3N2O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BCATc Inhibitor 2


BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively[1].

 Names

Name 5-Chloro-N'-{[2-(trifluoromethyl)phenyl]sulfonyl}-1-benzofuran-2-carbohydrazide
Synonym More Synonyms

 BCATc Inhibitor 2 Biological Activity

Description BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively[1].
Related Catalog
Target

IC50: 0.2 μM (rBCATc), 0.8 μM (hBCATc), 3.0 μM (rBCATm)[1].

In Vitro BCATc Inhibitor 2 decreases calcium influx in neuronal cultures with an IC50=4.8±1.2 μM[1].
In Vivo BCATc Inhibitor 2 also blocks calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrates neuroprotective efficacy in vivo[1]. Following a 30 mg/kg subcutaneous injection to Lewis rats, BCATc Inhibitor 2 reaches a peak plasma concentration (Cmax) of 8.28 μg/mL at 0.5 h (tmax). The mean plasma exposure (AUC) value is 19.9 μg h/mL, and the mean terminal half-life ranged from 12 to 15 h, indicating favorable PK parameters of BCATc Inhibitor 2[1].
References

[1]. Lain-Yen Hu, et al. The Design and Synthesis of Human Branched-Chain Amino Acid Aminotransferase Inhibitors for Treatment of Neurodegenerative Diseases. Bioorg Med Chem Lett. 2006 May 1;16(9):2337-40.

 Chemical & Physical Properties

Molecular Formula C16H10ClF3N2O4S
Molecular Weight 418.77

 Synonyms

2-Benzofurancarboxylic acid, 5-chloro-, 2-[[2-(trifluoromethyl)phenyl]sulfonyl]hydrazide
5-Chloro-N'-{[2-(trifluoromethyl)phenyl]sulfonyl}-1-benzofuran-2-carbohydrazide