1346233-68-8
- CAS号:1346233-68-8
- 英文名:3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-diMethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]Methyl]-benzaMide
- 中文名:1346233-68-8
- CBNumber:CB52695162
- 分子式:C19H26Cl2N2O
- 分子量:369.33
- MOL File:1346233-68-8.mol
- 沸点 :455.5±35.0 °C(Predicted)
- 密度 :1.184±0.06 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble10mg/mL (clear solution)
- 酸度系数(pKa) :13.65±0.46(Predicted)
- 形态 :powder
- 颜色 :white to beige
- WGK Germany :3
1346233-68-8性质、用途与生产工艺
- 生物活性 ML218 是一种有效的，选择性的和口服活性的 T 型 Ca2+ 通道 (Cav3.1，Cav3.2，Cav3.3) 抑制剂，对 Cav3.2 和 Cav3.3 的 IC50 分别为 310 nM 和 270 nM。ML218 抑制丘脑底核 (STN) 神经元的爆发活动。ML218 对 L 或 N 型钙通道，KATP 或 hERG 钾通道无明显抑制作用。ML218 可以穿透血脑屏障。
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靶点
IC50: 310 nM (Cav3.2), 270 nM (Cav3.3), and 150 nM (Ca 2+ flux)
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体外研究
In plasma protein binding studies (equilibrium dialysis), ML218 possesses good free fraction in both rat and human. Intrinsic clearance experiments in liver microsomes indicated that ML218 is highly cleared in rat (CL int = 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CL int = 12.7 mL/min/kg).
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体内研究
ML218 (0.03-30 mg/kg; oral administration; once; male Sprague-Dawley rats) treatment reverses cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol.
Free brain and plasma concentrations of ML218 increases in a dose proportional manner across the dose range (3 mg/kg: [plasma] = 98 nM, [brain] = 1.66 μM; 10 mg/kg: [plasma] = 282 nM, [brain] = 5.03 μM; 30 mg/kg: 1.2 μM, [brain] = 17.7 μM).
Noncompartmental pharmacokinetic analysis indicates ML218 (1 mg/kg, IV) has a mean residence time (MRT) of nearly 7 h, a value which is consistent with its terminal half-life (t 1/2 = 7 h).Animal Model: Male Sprague-Dawley rats (275-299 g) induced by haloperidol Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Oral administration; once Result: Reversed cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol.
- 更新日期：2024/11/08
- 产品编号：HY-103309
- 产品名称：ML218
- CAS编号：
- 包装：1 mg
- 价格：818元
- 更新日期：2024/11/08
- 产品编号：HY-103309
- 产品名称：1346233-68-8 ML218
- CAS编号：1346233-68-8
- 包装：5mg
- 价格：1800元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
