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BCATc Inhibitor 2 (Synonyms: Cytosolic Branched-Chain Amino Acid Transferase Inhibitor 2)

Catalog No.GC12912

cytosolic BCAT (BCATc) inhibitor

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BCATc Inhibitor 2 Chemical Structure

Cas No.: 406191-34-2

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50mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

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Background

BCATc Inhibitor 2 is an active and selective inhibitor of cytosolic BCAT (BCATc)[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].

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].

References:
[1] Hu L Y, Boxer P A, Kesten S R, et al.  The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases[J]. Bioorganic & medicinal chemistry letters, 2006, 16(9): 2337-2340.
[2] Brosnan J T, Brosnan M E.  Branched-chain amino acids: enzyme and substrate regulation[J]. The Journal of nutrition, 2006, 136(1): 207S-211S.

Chemical Properties

Cas No. 406191-34-2 SDF
Synonyms Cytosolic Branched-Chain Amino Acid Transferase Inhibitor 2
Chemical Name 5-chloro-2-benzofurancarboxylic acid 2-[[2-(trifluoromethyl)phenyl]sulfonyl]hydrazide
Canonical SMILES ClC1=CC=C2C(C=C(C(NNS(C3=C(C(F)(F)F)C=CC=C3)(=O)=O)=O)O2)=C1
Formula C16H10ClF3N2O4S M.Wt 418.8
Solubility ≤10mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide Storage Store at -20°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3878 mL 11.9389 mL 23.8777 mL
5 mM 0.4776 mL 2.3878 mL 4.7755 mL
10 mM 0.2388 mL 1.1939 mL 2.3878 mL
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