ML218|cas:1346233-68-8|西域试剂

ML218,99.49%

产品编号：Bellancom-103309| CAS NO：1346233-68-8| 分子式：C₁₉H₂₆Cl₂N₂O| 分子量：369.33

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-103309	￥1800.00	杭州北京（现货）
Bellancom-103309	￥2800.00	杭州北京（现货）
Bellancom-103309	￥9100.00	杭州北京（现货）
Bellancom-103309	￥14500.00	杭州北京（现货）

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ML218

产品介绍

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，K_ATP 或 hERG 钾通道无明显抑制作用。ML218 可以穿透血脑屏障。

生物活性

ML218 is a potent, selective and orally active T-type Ca²⁺ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, K_ATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (338.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7076 mL	13.5380 mL	27.0761 mL
5 mM	0.5415 mL	2.7076 mL	5.4152 mL
10 mM	0.2708 mL	1.3538 mL	2.7076 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (16.92 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (16.92 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。