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ML218

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Catalog No. T12076LCas No. 1346233-68-8

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).

ML218

ML218

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Purity: 99.45%
Catalog No. T12076LCas No. 1346233-68-8
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$52-In Stock
5 mg$123In StockIn Stock
10 mg$197In StockIn Stock
25 mg$358-In Stock
50 mg$517-In Stock
1 mL x 10 mM (in DMSO)$162-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.45%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
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
Cav 3.2:310 nM, Cav3.3:270 nM, 270 nM:Ca2+ flux
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].
Chemical Properties
Molecular Weight369.33
FormulaC19H26Cl2N2O
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 & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (270.76 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 5 mg/mL (13.54 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7076 mL13.5380 mL27.0761 mL135.3803 mL
5 mM0.5415 mL2.7076 mL5.4152 mL27.0761 mL
10 mM0.2708 mL1.3538 mL2.7076 mL13.5380 mL
20 mM0.1354 mL0.6769 mL1.3538 mL6.7690 mL
50 mM0.0542 mL0.2708 mL0.5415 mL2.7076 mL
100 mM0.0271 mL0.1354 mL0.2708 mL1.3538 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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