Apinocaltamide (C09-1102-250)

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 epilepsiesIn VitroApinocaltamide (Compound 66b) blocks Ca v 3.1, Ca v 3.2, Ca v 3.3, Ca v 1.2 with IC 50 s of 6.4, 18, 7.5 and 2410 nM, respectively. Apinocaltamide blocks recombinant channel hCa v 3.3 potently with marked voltage-dependency (K r ≈1500 nM and K i ≈20 nM). Apinocaltamide blocks currents through hK v 11.1-hERG channels with an IC 50 of 5.5 μM. Apinocaltamide also inhibits P450 enzymes with IC 50 s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoApinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) potently decreases the cumulative duration of absence-like seizures in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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%.Form:SolidIC50& Target:Ca v 1.2 2410 nM (IC 50 ) Ca V 3.1 6.4 nM (IC 50 ) Ca v 3.2 18 nM (IC 50 ) Ca V 3.3 7.5 nM (IC 50 ). Specifications and Purity: 99%. Molecular Formula: C22H18F3N5O. Molecular Weight: 425.41. PubChem CID: 118560618. Isomeric SMILES: C1CC1(C2=CC=C(C=C2)CC(=O)NC3=NN(C=C3)CC4=NC=C(C=C4)C#N)C(F)(F)F.