Chemical Structure : ACT 709478
CAS No.: 1838651-58-3
Catalog No.: 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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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.).
M.Wt | 425.415 | |
Formula | C22H18F3N5O | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)-phenyl)acetamide |
1. Bezençon O, et al. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b01236.
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