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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -ACT 709478
ACT 709478

Chemical Structure : ACT 709478

CAS No.: 1838651-58-3

ACT 709478 (Apinocaltamide, ACT709478)

货号: PC-62008Not For Human Use, Lab Use Only.

Apinocaltamide (ACT 709478) is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Apinocaltamide (ACT 709478) is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively.
ACT 709478 displays >100-fold selectivity over Cav1.2 channels.
ACT 709478 shows a significant decrease of the seizure severity in vivo (100 mg/kg, p.o.).

物理化学性质&存储条件

分子量 425.415
分子式 C22H18F3N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)-phenyl)acetamide

参考文献

1. Bezençon O, et al. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b01236.

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