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Basmisanil (Alias: RO5186582, RG1662)

Name: Basmisanil
Brand: TargetMol
SKU: T7165
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T7165 Copy Product Info

Purity: 99.42%

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Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.

Basmisanil

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Catalog No. T7165

Alias RO5186582, RG1662

Cas No. 1159600-41-5

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Pack Size	Price	USA Stock	Global Stock
2 mg	$32	In Stock	In Stock
5 mg	$51	In Stock	In Stock
10 mg	$72	In Stock	In Stock
25 mg	$125	In Stock	In Stock
50 mg	$207	In Stock	In Stock
100 mg	$396	In Stock	In Stock
500 mg	$892	-	In Stock
1 mL x 10 mM (in DMSO)	$44	In Stock	In Stock

In stock · 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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Batch Information

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Purity:99.42%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Basmisanil AI Summary

Basmisanil exhibits diverse bioactivities, particularly targeting GABA-A receptors and SARS-CoV-2. It shows a high binding affinity to various GABA-A receptor subunits, notably alpha1, alpha2, alpha3, and alpha5, with Ki values reaching 4.4 nM for the alpha5 subunit. The compound functions as a negative allosteric modulator at the alpha5 and alpha1 subunits, decreasing activity significantly at different concentrations. In antiviral studies, Basmisanil demonstrated moderate inhibitory activity against the SARS-CoV-2 3CL-Pro protease, with a 10.94% inhibition at 20µM concentration, and minimal inhibition of SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10µM after 48 hours of exposure. Additionally, the compound's impact on cell viability varies across different cell lines, promoting growth in HEK293T and U2OS cells while showing mixed effects in human fibroblast cells. Basmisanil also demonstrates moderate metabolic stability in both human and Wistar rat liver microsomes..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.
Synonyms	RO5186582, RG1662

Chemical Properties

Molecular Weight	445.46
Formula	C₂₁H₂₀FN₃O₅S
Cas No.	1159600-41-5
Smiles	Cc1onc(c1COc1ccc(cn1)C(=O)N1CCS(=O)(=O)CC1)-c1ccc(F)cc1
Relative Density.	1.388 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 32 mg/mL (71.84 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.49 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

	1mg	5mg	10mg	50mg
1 mM	2.2449 mL	11.2244 mL	22.4487 mL	112.2435 mL
5 mM	0.4490 mL	2.2449 mL	4.4897 mL	22.4487 mL
10 mM	0.2245 mL	1.1224 mL	2.2449 mL	11.2244 mL
20 mM	0.1122 mL	0.5612 mL	1.1224 mL	5.6122 mL
50 mM	0.0449 mL	0.2245 mL	0.4490 mL	2.2449 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.

Calculator

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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