1838651-58-3

Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies[1].

ChEBI: Apinocaltamide is a secondary carboxamide resulting from the formal condensation of the carboxy group of {4-[1-(trifluoromethyl)cyclopropyl]phenyl}acetic acid with the amino group of 6-[(3-amino-1H-pyrazol-1-yl)methyl]pyridine-3-carbonitrile. It is a selective, orally available T-type calcium channel blocker that is being studied as a potential new treatment in epilepsy. It has a role as an anticonvulsant and a T-type calcium channel blocker. It is a member of pyrazoles, a secondary carboxamide, a member of cyclopropanes, an organofluorine compound, a nitrile, a member of pyridines and a member of benzenes.

Ca_v1.2: 2410 nM (IC₅₀); Ca_V3.1: 6.4 nM (IC₅₀); Ca_v3.2: 18 nM (IC₅₀); Ca_V3.3: 7.5 nM (IC₅₀)

Store at -20°C

[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. DOI:10.1021/acs.jmedchem.7b01236