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ML218

Catalog No. T12076L CAS 1346233-68-8

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

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ML218, CAS 1346233-68-8

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Purity: 98%

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Description	ML218 inhibits the burst activity in the subthalamic nucleus (STN) neurons. ML218 is an effective, selective, and orally active inhibitor of T-type Ca2+ channel (Cav3.1, Cav3.2, Cav3.3) (IC50s: 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively). ML218 can penetrate the blood-brain barrier. ML218 has no significant inhibition of L- or N-type calcium channels, KATP, or hERG potassium channels.
Targets&IC50	Cav3.3:270 nM, Ca2+ flux:150 nM, Cav3.2:310 nM
In vitro	Intrinsic clearance experiments in liver microsomes indicated that ML218 is highly cleared in the rat (CLint = 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CLint = 12.7 mL/min/kg). ML218 possesses good free fraction in both rat and human, in plasma protein binding studies (equilibrium dialysis) .
In vivo	ML218 (0.03-30 mg/kg; oral administration; once; male Sprague-Dawley rats) treatment reverses cataleptic behavior in rats caused by a 0.75 mg/kg dose of haloperidol. 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). Free brain and plasma concentrations of ML218 enhances 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).

Molecular Weight	369.33
Formula	C19H26Cl2N2O
CAS No.	1346233-68-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Keywords

ML218 1346233-68-8 免疫与炎症微生物学 CCR ML-218 Inhibitor inhibitor inhibit

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