貨號	規格	價格	上海	北京	武漢	南京	購買數量
S82918-5mg	≥99%	￥2100.00 S82918-5mg ￥2100.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier

產品描述：

靶點：

IC50: 310 nM (Cav3.2), 270 nM (Cav3.3), and 150 nM (Ca2+ flux);CalciumChannel

體內研究：

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 (t1/2 = 7 h)

參考文獻：

1. Xiang Z, et al. The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742.

溶解性：

Soluble in DMSO

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.708 ml	13.538 ml	27.076 ml
5 mM	0.542 ml	2.708 ml	5.415 ml
10 mM	0.271 ml	1.354 ml	2.708 ml
50 mM	0.054 ml	0.271 ml	0.542 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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ML218

3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-benzamid