Zaldaride马来酸盐

Zaldaride马来酸盐用途

Zaldaride maleate (CGS-9343B) 是一个有效的、选择性的钙调蛋白 (calmodulin) 的抑制剂,可抑制钙调蛋白刺激cAMP磷酸二酯酶的活性,IC50 值为 3.3 nM。Zaldaride maleate (CGS-9343B) 可抑制雌激素诱导的ER转录激活,可逆地阻断PC12细胞中电压激活的的Na+、Ca2+和K+电流,抑制nAChR。

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Zaldaride马来酸盐名称

[ CAS 号 ]:
109826-27-9

[ 中文名 ]:
Zaldaride马来酸盐

[ 英文名 ]:
CGS 9343B

Zaldaride马来酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 3.3 nM (calmodulin)[1][2].

[参考文献]

[1]. Norman JA, et al. CGS 9343B, a novel, potent, and selective inhibitor of calmodulin activity. Mol Pharmacol. 1987 May;31(5):535-40.

[2]. Neuhaus R, et al. Inhibition of membrane currents and rises of intracellular Ca2+ in PC12 cells by CGS 9343B, a calmodulin inhibitor. Eur J Pharmacol. 1992 Jun 5;226(2):183-5.

[3]. Li L, et al. Calmodulin regulates the transcriptional activity of estrogen receptors. Selective inhibition of calmodulin function in subcellular compartments. J Biol Chem. 2003 Jan 10;278(2):1195-200.

Zaldaride马来酸盐物理化学性质

[ 密度 ]:
1.31g/cm3

[ 沸点 ]:
778ºC at 760 mmHg

[ 分子式 ]:
C₃₀H₃₂N₄O₆

[ 分子量 ]:
544.60

[ 闪点 ]:
424.3ºC

[ 精确质量 ]:
544.23200

[ PSA ]:
129.79000

[ LogP ]:
3.85250

[ 蒸汽压 ]:
1.78E-25mmHg at 25°C

[ 储存条件 ]:
2-8°C，干燥，密封

Zaldaride马来酸盐MSDS

详细MSDS(安全技术说明书)

Zaldaride马来酸盐安全信息

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

Zaldaride马来酸盐文献

Calcium Signaling Is Required for Erythroid Enucleation.

PLoS ONE 11 , e0146201, (2016)

Although erythroid enucleation, the property of erythroblasts to expel their nucleus, has been known for 7ore than a century, surprisingly little is known regarding the molecular mechanisms governing ...

The calmodulin inhibitor CGS 9343B inhibits voltage-dependent K(+) channels in rabbit coronary arterial smooth muscle cells.

Toxicol. Appl. Pharmacol. 285 , 207-13, (2015)

We investigated the effects of the calmodulin inhibitor CGS 9343B on voltage-dependent K(+) (Kv) channels using whole-cell patch clamp technique in freshly isolated rabbit coronary arterial smooth mus...

ATP hydrolysis is critically required for function of CaV1.3 channels in cochlear inner hair cells via fueling Ca2+ clearance.

J. Neurosci. 34(20) , 6843-8, (2014)

Sound encoding is mediated by Ca(2+) influx-evoked release of glutamate at the ribbon synapse of inner hair cells. Here we studied the role of ATP in this process focusing on Ca(2+) current through Ca...

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