| Identification | Back Directory | [Name]
ACT 709478 | [CAS]
1838651-58-3 | [Synonyms]
ACT 709478
apinocaltamide
ACT 709478
(ACT709478)
ACT-709478 1838651-58-3
Benzeneacetamide, N-[1-[(5-cyano-2-pyridinyl)methyl]-1H-pyrazol-3-yl]-4-[1-(trifluoromethyl)cyclopropyl]- | [Molecular Formula]
C22H18F3N5O | [MOL File]
1838651-58-3.mol | [Molecular Weight]
425.41 |
| Chemical Properties | Back Directory | [Boiling point ]
646.4±55.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:125.0(Max Conc. mg/mL);293.83(Max Conc. mM) | [form ]
A solid | [pka]
13.52±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Definition]
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. | [in vivo]
Apinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) potently decreases the cumulative duration of absence-like seizures in mice[1]. | Animal Model: | Male juvenile DBA/2J mice (22-24 days old)[1] | | Dosage: | 100, 300 mg/kg, 1 hour or 3 hours before exposure to the stimulus. | | Administration: | P.O., for 12 hours | | Result: | Decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%. |
| [IC 50]
Cav1.2: 2410 nM (IC50); CaV3.1: 6.4 nM (IC50); Cav3.2: 18 nM (IC50); CaV3.3: 7.5 nM (IC50) | [storage]
Store at -20°C | [References]
[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 |
|
|