2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. ML218 hydrochloride

ML218 hydrochloride 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 hydrochloride 抑制丘脑底核 (STN) 神经元的爆发活动。ML218 hydrochloride 对 L 或 N 型钙通道，KATP 或 hERG 钾通道无明显抑制作用。ML218 hydrochloride 可以穿透血脑屏障。

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ML218 hydrochloride Chemical Structure

ML218 hydrochloride Chemical Structure

CAS No. : 2319922-08-0

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ML218 hydrochloride 的其他形式现货产品:

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ML218 hydrochloride 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ML218 hydrochloride 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 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier[1].

IC50 & Target

IC50: 310 nM (Cav3.2), 270 nM (Cav3.3), and 150 nM (Ca2+ flux)[1]
体外研究
(In Vitro)

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 (CLint = 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CLint = 12.7 mL/min/kg)[1].

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

ML218 hydrochloride 相关抗体:
体内研究
(In Vivo)

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[1].
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)[1].
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 (t1/2 = 7 h)[1].

MCE 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[1]
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.
分子量

405.79

Formula

C19H27Cl3N2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ML218 hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML2182319922-08-0ML 218ML-218Calcium ChannelCa2+ channelsCa channelsT-typeCav3.1Cav3.2Cav3.3CNSsubthalamicnucleusoralneuronsParkinson’sdiseaseInhibitorinhibitorinhibit

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ML218 hydrochloride
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HY-103309A
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