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ML218 is an orally active, selective, potent, and blood-brain barrier-crossing inhibitor of T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) (IC50 for Cav3.2 and Cav3.3 is 310 nM and 270 nM, respectively).ML218 inhibits the burst activity of neurons in the subthalamic nucleus (STN).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
50 mg | $755 | 6-8 weeks | |
100 mg | $1,190 | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $196 | 6-8 weeks |
Description | ML218 is an orally active, selective, potent, and blood-brain barrier-crossing inhibitor of T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) (IC50 for Cav3.2 and Cav3.3 is 310 nM and 270 nM, respectively).ML218 inhibits the burst activity of neurons in the subthalamic nucleus (STN). |
Targets&IC50 | 270 nM:Ca2+ flux, Cav3.3:270 nM, Cav 3.2:310 nM |
In vitro | In a voltage clamp experiment, bath application of 3 μM ML218 significantly reduced the T-type Ca2+ current by ∼45%[1]. |
In vivo | In Male Sprague-Dawley rats (275-299 g) induced by haloperidol,ML218 (0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg; Oral administration; once) treatment reversed cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol[1]. |
Molecular Weight | 369.33 |
Formula | C19H26Cl2N2O |
Cas No. | 1346233-68-8 |
Smiles | [H][C@@]12CN(CCC(C)(C)C)C[C@]1([H])[C@H]2CNC(=O)c1cc(Cl)cc(Cl)c1 |
Relative Density. | 1.184 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (270.76 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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