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GS 39783

Name: GS 39783
Brand: TargetMol
SKU: T22813
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22813Cas No. 39069-52-8

GS 39783 is a positive allosteric modulator (PAM) of GABABR, which reduces the motivational properties of alcohol and the conditioned reinforcement and conditional reward of psychostimulants.

GS 39783

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Purity: 99.92%

Catalog No. T22813Cas No. 39069-52-8

GS 39783 is a positive allosteric modulator (PAM) of GABABR, which reduces the motivational properties of alcohol and the conditioned reinforcement and conditional reward of psychostimulants.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$32	-	In Stock
5 mg	$53	-	In Stock
10 mg	$83	-	In Stock
25 mg	$158	-	In Stock
50 mg	$257	-	In Stock
100 mg	$373	-	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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Batch Information

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Purity:99.92%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR HPLC

Product Introduction

GS 39783 AI Summary

GS 39783 exhibits a diverse range of bioactivities across various assays and biological systems. It acts as a positive allosteric modulator of GABAB receptors, particularly GABA-B1 and GABA-B1b, expressed in CHO-K1 cells and rat cortical membranes, showing an EC50 of 741.31 nM and modulation efficacy between 132.0% and 192.0%. Additionally, it modulates GABA activity, with a recorded Emax of 146.0% when co-administered with 1 µM GABA. The compound also displays inhibition of critical enzymes and interactions: - Menin-MLL interaction in leukemia (potency: 39810.7 nM) - Tyrosyl-DNA Phosphodiesterase (TDP1) (potency: 891.3 nM) - Cytochrome P450 enzymes (2C19 and 2C9) (potencies: 5011.9 nM and 1995.3 nM, respectively) - USP1/UAF1 (potency: 15848.9 nM) - Anthrax Lethal Toxin Internalization (potency: 10000.0 nM) Its antiviral capabilities are demonstrated by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, though with varying degrees of efficacy. Additionally, the compound inhibits SARS-CoV-2 3CL-Pro protease at 20 µM. In hypnotic assays with DBA mice, GS 39783 increases the pentobarbital-induced duration and reduces onset time of the loss of the righting reflex. However, it shows cytotoxicity in mouse NIH/3T3 cells with an IC50 of 60000.0 nM. In GPCR beta-arrestin recruitment assays, it exhibits varying degrees of modulation across multiple targets, implicating potential effects on diverse receptor systems. Moreover, thermal shift assays suggest both stabilizing and destabilizing effects on protein structures, indicating complex interactions with protein domains. Lastly, GS 39783 displays inhibition of human HDAC6 activity, with a higher inhibition percentage using commercial substrates (47.7%) compared to custom ones (5.72%), and depending on cell type, it shows differential impacts on cell viability: generally promoting growth in HEK293T cells, mixed effects in U2OS cells, and varying effects in human fibroblast cells..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

GS 39783 is a positive allosteric modulator (PAM) of GABABR, which reduces the motivational properties of alcohol and the conditioned reinforcement and conditional reward of psychostimulants.

Chemical Properties

Molecular Weight	337.44
Formula	C₁₅H₂₃N₅O₂S
Cas No.	39069-52-8
Smiles	N(C=1C(N(=O)=O)=C(NC2CCCC2)N=C(SC)N1)C3CCCC3
Relative Density.	1.31g/cm3

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

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 20 mg/mL (59.27 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.93 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	2.9635 mL	14.8174 mL	29.6349 mL	148.1745 mL
5 mM	0.5927 mL	2.9635 mL	5.9270 mL	29.6349 mL
10 mM	0.2963 mL	1.4817 mL	2.9635 mL	14.8174 mL
20 mM	0.1482 mL	0.7409 mL	1.4817 mL	7.4087 mL
50 mM	0.0593 mL	0.2963 mL	0.5927 mL	2.9635 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:

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