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

ML218 hydrochloride 

Cat. No.: HY-103309A
Handling Instructions

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.

For research use only. We do not sell to patients.

ML218 hydrochloride Chemical Structure

ML218 hydrochloride Chemical Structure

CAS No. : 2319922-08-0

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Description

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]

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].

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].

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.
Molecular Weight

405.79

Formula

C₁₉H₂₇Cl₃N₂O

CAS No.

2319922-08-0

SMILES

O=C(NC[[email protected]@H]1[[email protected]@]2([H])CN(CCC(C)(C)C)C[[email protected]@]12[H])C3=CC(Cl)=CC(Cl)=C3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ML218ML 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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