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BCATc Inhibitor 2

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Purity:97.99%

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COA HNMR LCMS

BCATc Inhibitor 2

Catalog No. T22043Cas No. 406191-34-2

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective efficacy in vivo[1]. Branched-chain amino acid transferases (BCATs) have been implicated in catalyzing reversible transamination of isoleucine, leucine, and valine branched-chain amino acids to their corresponding α-keto acids, generating L-glutamate. It has been identified that there are two forms of BCAT in mammals: mitochondrial BCAT (BCATm) and cytosolic BCAT (BCATc). BCATc is expressed in particular brain region and involved in regulating glutamate synthesis for release during neuronal excitation. Thus, BCATc inhibition may be useful for the treatment of neurodegenerative and behavioral disorders involving disturbances of the glutamatergic system [2].

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Pack Size	Price	Availability
1 mg	$51	In Stock
2 mg	$74	In Stock
5 mg	$122	In Stock
10 mg	$197	In Stock
25 mg	$413	In Stock
50 mg	$618	In Stock
100 mg	$879	In Stock
1 mL x 10 mM (in DMSO)	$147	In Stock

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Product Introduction

Bioactivity

Description	BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e
In vitro	BCATc inhibition is likely to be useful for the treatment of neurodegenerative and other neurological disorders involving disturbances of the glutamatergic system. In the hBCATc assays, BCATc Inhibitor 2 exhibited an IC50 of 0.8 ± 0.05 μM. In a recombinant rat BCATc assay and a crude rat BCATm assay, the IC50 was 0.2 μM ± 0.02 and 3.0 μM ± 0.5 (n=5), respectively. BCATc Inhibitor 2 decreased calcium influx in neuronal cultures with an IC50 of 4.8 ± 1.2 μM (n=4) [1].
In vivo	BCATc Inhibitor 2 blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective efficacy in vivo. In Lewis rats, after treatment with 30 mg/kg BCATc Inhibitor 2 (subcutaneous injection), the peak plasma concentration (Cmax) reached 8.28 μg/ml at 0.5 h (tmax). The mean plasma exposure (AUC) value was 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. Daily administration of the mitochondrial neurotoxin, 3-nitroproprionic acid (3-NP) produced striatal lesions and led to motor deficits. Administration of BCATc Inhibitor 2 for 9 days almost completely reversed the effects of 3-NP [1].

Chemical Properties

Molecular Weight	418.77
Formula	C16H10ClF3N2O4S
Cas No.	406191-34-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 65 mg/ml (155.22 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3879 mL	11.9397 mL	23.8795 mL	119.3973 mL
5 mM	0.4776 mL	2.3879 mL	4.7759 mL	23.8795 mL
10 mM	0.2388 mL	1.1940 mL	2.3879 mL	11.9397 mL
20 mM	0.1194 mL	0.5970 mL	1.1940 mL	5.9699 mL
50 mM	0.0478 mL	0.2388 mL	0.4776 mL	2.3879 mL
100 mM	0.0239 mL	0.1194 mL	0.2388 mL	1.1940 mL

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