| 货号 | 9002002-1mg |
| 描述 | Branched-chain amino acid transferases (BCATs) catalyze reversible transamination of leucine, isoleucine, and valine branched-chain amino acids to their respective α-keto acids, liberating L-glutamate.1,2 Two forms of BCAT are present in mammals. Mitochondrial BCAT (BCATm) exists in most tissues throughout the body, whereas cytosolic BCAT (BCATc) is confined to the brain, where it regulates 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. BCATc Inhibitor 2 is a sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM for human and rat, respectively) with 15-fold selectivity over BCATm.3,4,5 This compound has been shown to block calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and to demonstrate neuroprotective efficacy in an in vivo rat model of neurodegeneration.4 |
| 别名 | Cytosolic Branched-Chain Amino Acid Transferase Inhibitor 2; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Brosnan, J.T., and Brosnan, M.E. Branched-chain amino acids: Enzyme and substrate regulation. Journal of Nutrition 136(1), 207S-211S (2006). 2.Goto, M.,Miyahara, I.,Hayashi, H., et al. Crystal structures of branched-chain amino acid aminotransferase complexed with glutamate and glutarate: True reaction intermediate and double substrate recognition of the enzyme. Biochem. 42, 3725-3733 (2003). 3.Bora, K.,Hu, L.Y.,Kesten, S.R., et al. Branched chain amino acid-dependent aminotransferase inhibitors and their use in the treatment of neurodegenerative diseases. PCT/US01/25892, (2002). 4.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. Bioorganic & Medicinal Chemistry Letters 16(9), 2337-2340 (2006). 5.Caballero, J.,Vergara-Jaque, A.,Fernández, M., et al. Docking and quantitative structure-activity relationship studies for sulfonyl hydrazides as inhibitors of cytosolic human branched-chain amino acid aminotransferase. Mol.Divers. 13(4), 493-500 (2009). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 418.8 |
| 分子式 | C16H10ClF3N2O4S |
| CAS号 | 406191-34-2 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |