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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
ACT-709478
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1838651-58-3
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2090.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥863.0 |
| 规格： | 5 mg | 产品价格： | ￥1900.0 |
| 规格： | 10 mg | 产品价格： | ￥2900.0 |
| 规格： | 25 mg | 产品价格： | ￥4500.0 |
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Apinocaltamide
CAS No. : 1838651-58-3
MCE 国际站：Apinocaltamide
产品活性：Apinocaltamide (ACT-709478) 是一种口服有效的，可透过血脑屏障的选择性 T 型电压门控钙通道 (T-type calcium channel) 阻滞剂，可用于全身性癫痫的研究。
研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：Calcium Channel
In Vitro: 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.
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.
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