| Bioactivity | 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]. | ||||||||||||
| Invitro | Apinocaltamide (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. Apinocaltamide blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). Apinocaltamide blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1].Apinocaltamide also inhibits P450 enzymes with IC50s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively[1]. | ||||||||||||
| 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: | ||||||||||||
| Name | Apinocaltamide | ||||||||||||
| CAS | 1838651-58-3 | ||||||||||||
| Formula | C22H18F3N5O | ||||||||||||
| Molar Mass | 425.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Bezençon 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. |
Apinocaltamide
CAS: 1838651-58-3 F: C22H18F3N5O W: 425.41
Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker.
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.