ACT 709478

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ACT 709478 是一种有效的、选择性的、口服生物可利用的、脑渗透性 T 型钙通道阻滞剂，对 Cav3.1、Cav3.2 和 Cav3.3 通道的 IC50 分别为 6.4、18 和 7.5 nM。

ACT 709478 is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively; displays >100-fold selectivity over Cav1.2 channels; shows a significant decrease of the seizure severity in vivo (100 mg/kg, p.o.).Epilepsy Phase 2 Clinical.

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.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.

Apinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) 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%.

ACT709478

GPCR/G Protein

Calcium Channel

Calcium Channel

Neurological Disease

Epilepsy

1838651-58-3

425.415

C22H18F3N5O

>98% (HPLC)

DMSO : ≥ 125 mg/mL 293.83 mM

O=C(NC1=NN(CC2=NC=C(C#N)C=C2)C=C1)CC3=CC=C(C4(C(F)(F)F)CC4)C=C3

N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)-phenyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years