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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。
ACT-709478图片
CAS NO:1838651-58-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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 SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.