CGP 37157
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CGP 37157是一种强效的和选择性的线粒体Na +-Ca2 +交换拮抗剂,IC50值为0.4 μM[1].
线粒体Na +-Ca2 +交换(mNCE)是一种逆向转运膜蛋白,输出一个Ca2 +以引入三个Na +.线粒体Ca2 +摄取在控制细胞凋亡\调节代谢活性和Ca2 +形成以及Ca2 +信号的缓冲中起关键作用[2].
CGP 37157是一种选择性mNCE拮抗剂.在离体心脏线粒体中,CGP-37157剂量依赖性地抑制mNCE的活性,IC 50值为0.36 μM[1].在人类和小鼠β细胞中,CGP-37157剂量依赖性地抑制KCl和葡萄糖刺激的Ca2 +信号,并降低灌流胰岛分泌胰岛素[2].在大鼠前脑神经元中,CGP-37157一致引起谷氨酸刺激的Ca2 +流入急剧下降,这表明谷氨酸诱导的Ca 2+流入恢复由mNCE调节[3].在大鼠背根神经节神经元中,CGP 37157抑制去极化诱导的Ca2 +内流和线粒体介导的Ca2 +内流[4].
参考文献:
[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.
Physical Appearance | A white to off- |
Storage | Store at RT |
M.Wt | 324.22 |
Cas No. | 75450-34-9 |
Formula | C15H11Cl2NOS |
Solubility | Soluble in DMSO |
Chemical Name | (R)-7-chloro-5-(2-chlorophenyl)-3,5-dihydrobenzo[e][1,4]thiazepin-2(1H)-one |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=CC=C1[C@@H](C2=C3)SCC(NC2=CC=C3Cl)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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