BCATc Inhibitor 2_product_DataBase

Bioactivity	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. BCATc, also called BCAT1, is in the cytoplasm[1].
Target	IC50: 0.2 μM (rBCATc), 0.8 μM (hBCATc), 3.0 μM (rBCATm).
Invitro	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].
Name	BCATc Inhibitor 2
CAS	406191-34-2
Formula	C16H10ClF3N2O4S
Molar Mass	418.77
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[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.

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