CGP 37157
目录号 : GC11630
A selective inhibitor of the mitochondrial sodium-calcium exchanger NCLX
Cas No.:75450-34-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cell toxicity assays are performed. Neurons are exposed to NMDA in HBSS (free of Ca2+ and Mg2+) containing 2.6 mM CaCl2, 10 mM glucose and 10 μM glycine for 10 or 30 min at 37°C, depending on the experiment. CGP37157 is present before and during the excitotoxic insult and cell viability is assessed 24 h later using Citotox 96 colorimetric assay. All experiments are performed in quadruplicate and the values provided are the normalized mean ± S.E.M. of at least three independent experiments[1]. |
References: [1]. Chiesi M, et al. Structural dependency of the inhibitory action of benzodiazepines and related compounds on the mitochondrial Na+-Ca2+ exchanger. Biochem Pharmacol. 1988 Nov 15;37(22):4399-403. | |
CGP 37157 is a potent and selective antagonist of the mitochondrial Na+-Ca2+ exchanger with IC50 value of 0.4 μM [1].
The mitochondrial Na+-Ca2+ exchanger (mNCE) is an antiporter membrane protein and removes a single Ca2+ in exchange for the import of three Na+. Mitochondrial Ca2+ uptake plays a critical role in the control of apoptosis, regulation of metabolic activity and Ca2+ shaping and buffering of Ca2+ signals [2].
CGP 37157 is a selective mNCE antagonist. In isolated heart mitochondria, CGP-37157 inhibited the activity of mNCE with IC50 value of 0.36 μM in a dose-dependent way [1]. In human and mouse β-cells, CGP-37157 inhibited KCl- and glucose-stimulated Ca2+ signals in a dose-dependent way and decreased insulin secretion from perifused islets [2]. In rat forebrain neurons, CGP-37157 consistently caused a rapid fall in Ca2+ influx stimulated by glutamate, which suggested the recovery of Ca2+ influx induced by glutamate was regulated via mNCE [3]. In rat dorsal root ganglion neurons, CGP37157 inhibited depolarization-induced Ca2+ influx and mitochondrion-mediated Ca2+ influx [4].
References:
[1]. Cox DA, Conforti L, Sperelakis N, et al. Selectivity of inhibition of Na(+)-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157. J Cardiovasc Pharmacol, 1993, 21(4): 595-599.
[2]. Luciani DS, Ao P, Hu X, et al. Voltage-gated Ca(2+) influx and insulin secretion in human and mouse beta-cells are impaired by the mitochondrial Na(+)/Ca(2+) exchange inhibitor CGP-37157. Eur J Pharmacol, 2007, 576(1-3): 18-25.
[3]. White RJ, Reynolds IJ. Mitochondria accumulate Ca2+ following intense glutamate stimulation of cultured rat forebrain neurones. J Physiol, 1997, 498 ( Pt 1): 31-47.
[4]. Baron KT, Thayer SA. CGP37157 modulates mitochondrial Ca2+ homeostasis in cultured rat dorsal root ganglion neurons. Eur J Pharmacol, 1997, 340(2-3): 295-300.
| Cas No. | 75450-34-9 | SDF | |
| 化学名 | (R)-7-chloro-5-(2-chlorophenyl)-3,5-dihydrobenzo[e][1,4]thiazepin-2(1H)-one | ||
| Canonical SMILES | ClC1=CC=CC=C1[C@@H](C2=C3)SCC(NC2=CC=C3Cl)=O | ||
| 分子式 | C15H11Cl2NOS | 分子量 | 324.22 |
| 溶解度 | DMSO: 100 mM,Ethanol: 25 mM | 储存条件 | Store at RT |
| 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 | 3.0843 mL | 15.4216 mL | 30.8433 mL |
| 5 mM | 0.6169 mL | 3.0843 mL | 6.1687 mL |
| 10 mM | 0.3084 mL | 1.5422 mL | 3.0843 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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