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Please store the product under the recommended conditions in the Certificate of Analysis.
- 库存:
货期:电询
- 供应商:
MedChemExpress LLC
- CAS号:
2319922-08-0
- 规格:
电询
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ML218 hydrochloride
CAS No. : 2319922-08-0
MCE 国际站:ML218 hydrochloride
产品活性: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。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:Calcium Channel
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).
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.
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).
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文献和实验Guanidine Hydrochloride Purification of Proteins From SDS
Pepstatin A (2.0 mg/ml)10 ml Leupeptin (1.0 mg/ml)10 ml Aprotinin (5.0 mg/ml)(Protease Inhibitor Cocktail Sigma #P8340)Denaturation Buffer6 M guanidine hydrochloride 57.3 g G-HCl20 mM Hepes 7.9 2 ml 1M Hepes pH 7.910 mM KCl 0.074 g KCl0.5 mM DTT 100 ml 0.5 M
Guanidine Hydrochloride Purification of Proteins From SDS PAGE
(Sigma #P7626) 10 ml Pepstatin A (2.0 mg/ml) 10 ml Leupeptin (1.0 mg/ml) 10 ml Aprotinin (5.0 mg/ml) (Protease Inhibitor Cocktail Sigma #P8340) Denaturation Buffer 6 M guanidine hydrochloride 57.3 g G-HCl 20 mM Hepes 7.9 2 ml 1M Hepes pH 7.9 10 mM
Zymolyase Dissolve in 10% glucose. Store aliquots (25 µl) at 20o C in common freezer for stock solutions Use once and dispose Comments: alternative is to dissolve in SCE, 40% gycerol, 20 mg/ml final. Can use
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