ACT-709478

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ACT-709478

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1838651-58-3

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
5mg	询价
10mg	询价
50mg	询价
100mg	询价

ACT-709478是一种有效、选择性、可口服、可透过血脑屏障的T型电压门控钙通道(T-typecalciumchannel)阻滞剂，对Cav3.1，Cav3.2，Cav3.3，Cav1.2的IC50值分别为6.4，18，7.5和2410nM。ACT-709478对大鼠、小鼠、狗和猕猴的T-typecalciumchannel都有作用，物种差异不大。ACT-709478可用于全身性癫痫的研究。

Cas No.	1838651-58-3
Canonical SMILES	O=C(NC1=NN(CC2=NC=C(C#N)C=C2)C=C1)CC3=CC=C(C4(C(F)(F)F)CC4)C=C3
分子式	C₂₂H₁₈F₃N₅O
分子量	425.41
溶解度	DMSO : ≥ 125 mg/mL (293.83 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	ACT-709478 is a potent, selective, oral active, and brain penetrating T-type calcium channel blocker, with IC50s of 6.4, 18, 7.5 and 2410 nM for Cav3.1, Cav3.2, Cav3.3, Cav1.2, respectively. ACT-709478 is effective on rat and mice, dog, and cynomolgus T-type calcium channel, with no significant species differences. ACT-709478 is used in the research of generalized epilepsies[1]. ACT-709478 (Compound 66b) blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1].ACT-709478 shows weak inhibition on P450, with IC50s of 52, 14, 22, 25, 15, and 51 μM for P4502A6, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4, respectively[1]. [1]. Bezen?on O, et al. Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. J Med Chem. 2017 Dec 14;60(23):9769-9789.