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.
IC50&Target
Cav3.1
6.4 nM (IC50)
Cav3.2
18 nM (IC50)
Cav3.3
7.5 nM (IC50)
Cav1.2
2410 nM (IC50)
体外研究
ACT-709478 (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. ACT-709478 blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). ACT-709478 blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM.
ACT-709478 also inhibits P450 enzymes with IC50s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively.
体内研究
ACT-709478 (Compound 66b, 100, 300 mg/kg, p.o., 12 hours) potently decreases the cumulative duration of absence-like seizures in mice.
Animal Model:
Male juvenile DBA/2J mice (22-24 days old)
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%.
分子式
C22H18F3N5O
分子量
425.41
CAS号
1838651-58-3
运输条件
Room temperature in continental US; may vary elsewhere.