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CL 218872

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Catalog No. T8572Cas No. 66548-69-4

CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxiolytic and anticonvulsant in vivo.

CL 218872

CL 218872

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🥰Excellent
Purity: 99.92%
Catalog No. T8572Cas No. 66548-69-4
CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxiolytic and anticonvulsant in vivo.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$35In StockIn Stock
50 mg$62In StockIn Stock
100 mg$103In StockIn Stock
1 mL x 10 mM (in DMSO)$29In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.92%
Appearance:Solid
Color:White
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Product Introduction

CL 218872 AI Summary
CL 218872 exhibits significant bioactivity across various systems, predominantly influencing GABAergic neurotransmission. It demonstrates binding affinities with multiple subunits of the GABA-A receptor, showing strong affinity particularly for the alpha-1-beta-3-gamma-2 subunits (Ki = 57.0 nM) and moderate affinities for other subunits such as alpha-3-beta-3-gamma-2 (Ki = 1161.0 nM) and alpha-5-beta-3-gamma-2 (Ki = 561.0 nM). It binds to various GABA-A receptor subtypes with Ki values ranging from 57.0 nM to greater than 10000.0 nM, indicating selective bioactivity towards certain subtypes. Additionally, CL 218872 exhibits anticonvulsant activity, demonstrated by its efficacy in preventing convulsions in mice, and shows anxiolytic properties by protecting against pentylenetetrazole-induced convulsions. Moreover, CL 218872 shows binding affinity for the benzodiazepine receptor (Ki = 198.0 nM) and relative binding to the central benzodiazepine receptor with a GABA ratio of 1.2 in the presence and absence of 10e-4 M GABA. This suggests potential modulation of GABAergic neurotransmission through interaction with benzodiazepine sites. In addition to its neurological activities, CL 218872 has shown inhibitory effects on various targets, including enzymes like Cytochrome P450 3A4, ALDH1A1, and HPGD, and it exhibits antiviral activity against SARS-CoV-2, providing broad pharmacological potential. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells and demonstrates modest inhibition of SARS-CoV-2 3CL-Pro protease. Overall, CL 218872 is a potent GABA-A receptor modulator with anticonvulsant and anxiolytic properties, alongside exhibiting significant enzymatic and antiviral bioactivities..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxiolytic and anticonvulsant in vivo.
Chemical Properties
Molecular Weight278.23
FormulaC13H9F3N4
Cas No.66548-69-4
SmilesCC=1N2C(C=CC(=N2)C3=CC(C(F)(F)F)=CC=C3)=NN1
Relative Density.1.43g/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: 13.9 mg/mL (49.96 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.5941 mL17.9707 mL35.9415 mL179.7074 mL
5 mM0.7188 mL3.5941 mL7.1883 mL35.9415 mL
10 mM0.3594 mL1.7971 mL3.5941 mL17.9707 mL
20 mM0.1797 mL0.8985 mL1.7971 mL8.9854 mL

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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.

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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.
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