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BCATc Inhibitor 2

产品编号 T22043 CAS 406191-34-2

BCATc Inhibitor 2 是选择性分支链氨基转移酶抑制剂，可用于神经退行性疾病的研究。能够抑制 rBCATc (IC50:0.2 μM)，hBCATc (IC50:0.8 μM)、 rBCATm (IC50:3.0 μM)。其中BCATc 也称为 BCAT1，存在于细胞质基质中的亚型。

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BCATc Inhibitor 2, CAS 406191-34-2

规格	价格/CNY	货期
1 mg	￥ 525	现货
2 mg	￥ 762	现货
5 mg	￥ 1,230	现货
10 mg	￥ 1,980	现货
25 mg	￥ 3,550	现货
50 mg	￥ 5,130	现货
100 mg	￥ 7,270	现货
1 mL * 10 mM (in DMSO)	￥ 1,450	现货

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选择批次

纯度: 97.99%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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].
靶点活性	BCATm (rat):3.0 μM (IC50), BCATc (rat):0.2 μM (IC50), BCATc (human):0.8 μM (IC50)
体外活性	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].
体内活性	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].

分子量	418.77
分子式	C16H10ClF3N2O4S
CAS No.	406191-34-2

存储

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

溶解度

DMSO: 65 mg/ml (155.22 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3879 mL	11.9397 mL	23.8795 mL	59.6986 mL
	5 mM	0.4776 mL	2.3879 mL	4.7759 mL	11.9397 mL
	10 mM	0.2388 mL	1.194 mL	2.3879 mL	5.9699 mL
	20 mM	0.1194 mL	0.597 mL	1.194 mL	2.9849 mL
	50 mM	0.0478 mL	0.2388 mL	0.4776 mL	1.194 mL
	100 mM	0.0239 mL	0.1194 mL	0.2388 mL	0.597 mL

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参考文献

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.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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