BCATc Inhibitor 2
(Synonyms: Cytosolic Branched-Chain Amino Acid Transferase Inhibitor 2) 目录号 : GC12912
A selective BCATc inhibitor
Cas No.:406191-34-2
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
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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.
| Cas No. | 406191-34-2 | SDF | |
| 别名 | Cytosolic Branched-Chain Amino Acid Transferase Inhibitor 2 | ||
| 化学名 | 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 | ||
| 分子式 | C16H10ClF3N2O4S | 分子量 | 418.8 |
| 溶解度 | ≤10mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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