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Licostinel (Synonyms: CGP-63446, CGP 63446, ACEA-1021, ACEA1021, ACEA 1021)

Catalog No. T27828 Copy Product Info
Purity: 98.02%
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Licostinel (CGP 63446) is a glutamate receptor antagonist. Licostinel protects against permanent focal cerebral ischemia.

Licostinel

Copy Product Info
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Catalog No. T27828
Synonyms CGP-63446, CGP 63446, ACEA-1021, ACEA1021, ACEA 1021

Licostinel (CGP 63446) is a glutamate receptor antagonist. Licostinel protects against permanent focal cerebral ischemia.

Licostinel
Cas No. 153504-81-5
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Pack SizePriceUSA StockGlobal StockQuantity
5 mg$33In StockIn Stock
10 mg$52In StockIn Stock
25 mg$110In StockIn Stock
50 mg$178In StockIn Stock
100 mg$266In StockIn Stock
1 mL x 10 mM (in DMSO)$35In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:98.02%
Appearance:Solid
Color:Yellow
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Product Introduction

Licostinel AI Summary
Licostinel exhibits a range of pharmacological effects and binding affinities. It shows a high affinity for the glycine binding site of the NMDA receptor, with IC50 values ranging from 1.4 nM to 5.9 nM in various assays. It demonstrates potent anticonvulsant activity, indicated by an effective dose of 3.3 mg/kg in protecting DBA/2 mice from audiogenic seizures, and an ED50 of 4.0 mg/kg in the mouse maximal electroshock (MES) assay. The compound also shows effectiveness in reducing nociception in vivo, with an ED50 of 5.0 mg/kg and an EC50 of 1000.0 nM in a formalin paw nociception model. Furthermore, it exhibits selectivity for the NMDA receptor glycine site over non-NMDA receptor sites and has a moderate binding affinity (Kb = 1500.0 nM) for the AMPA receptor. Licostinel has a partition coefficient (logP) of 0.21, suggesting good water solubility and favorable pharmacokinetic properties. Additionally, it has been shown to reduce infarct volumes in rat models of cerebral ischemia and inhibit glutamate-stimulated cyclic GMP accumulation in neonatal rat cerebral slices..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Licostinel (CGP 63446) is a glutamate receptor antagonist. Licostinel protects against permanent focal cerebral ischemia.
SynonymsCGP-63446, CGP 63446, ACEA-1021, ACEA1021, ACEA 1021
Chemical Properties
Molecular Weight276.03
FormulaC8H3Cl2N3O4
Cas No.153504-81-5
Smiles[O-][N+](=O)c1c(Cl)c(Cl)cc2[nH]c(=O)c(=O)[nH]c12
Relative Density.1.757g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (199.25 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.6228 mL18.1140 mL36.2279 mL181.1397 mL
5 mM0.7246 mL3.6228 mL7.2456 mL36.2279 mL
10 mM0.3623 mL1.8114 mL3.6228 mL18.1140 mL
20 mM0.1811 mL0.9057 mL1.8114 mL9.0570 mL
50 mM0.0725 mL0.3623 mL0.7246 mL3.6228 mL
100 mM0.0362 mL0.1811 mL0.3623 mL1.8114 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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