| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
GS39783 targets the GABA-B receptor, a G protein-coupled receptor that mediates inhibitory neurotransmission in the central nervous system. As a positive allosteric modulator, GS39783 binds to an allosteric site on the receptor and enhances the affinity and efficacy of the endogenous agonist GABA. This potentiates inhibitory neurotransmission.
|
|---|---|
| ln Vitro |
In vitro, GS39783 enhances GABA-B receptor-mediated signaling. Its activity is assessed by measuring its effects on GABA-induced G protein activation, calcium signaling, or other downstream readouts. The compound potentiates the effects of GABA without having intrinsic agonist activity.
|
| ln Vivo |
In vivo, GS39783 has been studied in animal models of anxiety, depression, and drug addiction. By potentiating GABA-B receptor signaling, the compound reduces anxiety-like behaviors and may decrease drug-seeking behaviors. It has potential applications in the treatment of psychiatric disorders.
|
| Enzyme Assay |
In vitro receptor binding assays for GS39783 measure its affinity for the GABA-B receptor allosteric site using radioligand displacement or functional assays. The compound's ability to potentiate GABA-induced signaling is assessed by measuring G protein activation, calcium flux, or cAMP modulation in cells expressing GABA-B receptors.
|
| Cell Assay |
In vitro cell-based assays for GS39783 use cells expressing GABA-B receptors. Cells are treated with serial dilutions of the compound, and GABA-B receptor-mediated signaling is measured. The EC50 for potentiation of GABA responses is calculated from dose-response curves. Cell viability is assessed in parallel.
|
| Animal Protocol |
In vivo animal models for GS39783 include models of anxiety (e.g., elevated plus maze), depression (e.g., forced swim test), and drug addiction (e.g., self-administration). The compound is administered orally or intraperitoneally, and its effects on behavior and drug-seeking are evaluated.
|
| ADME/Pharmacokinetics |
GS39783 has a molecular formula of C₁₄H₁₃Cl₂N₃OS and a molecular weight of 342.24 g/mol. It is soluble in DMSO and is stored at -20°C. The compound is a positive allosteric modulator of GABA-B receptors. It is intended for laboratory research use only.
|
| Toxicity/Toxicokinetics |
The toxicity profile of GS39783 is characterized in preclinical safety studies. As a GABA-B receptor PAM, the compound is generally well-tolerated at therapeutic doses. The compound is for research use only and is not approved for clinical use.
|
| References | |
| Additional Infomation |
N4,N6-Dicyclopentyl-2-(methylthio)-5-nitropyrimidine-4,6-diamine is an aryl thioether.
GS39783 is a positive allosteric modulator (PAM) of the GABA-B receptor. It enhances GABA-B receptor signaling without directly activating the receptor. GS39783 has been studied for potential applications in anxiety, depression, and drug addiction. It is intended for laboratory research use only. |
| Molecular Formula |
C15H23N5O2S
|
|---|---|
| Molecular Weight |
337.44
|
| Exact Mass |
337.157
|
| CAS # |
39069-52-8
|
| PubChem CID |
6604928
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.3g/cm3
|
| Boiling Point |
561.9ºC at 760 mmHg
|
| Flash Point |
293.7ºC
|
| Index of Refraction |
1.614
|
| LogP |
4.484
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
368
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GSGVDKOCBKBMGG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H23N5O2S/c1-23-15-18-13(16-10-6-2-3-7-10)12(20(21)22)14(19-15)17-11-8-4-5-9-11/h10-11H,2-9H2,1H3,(H2,16,17,18,19)
|
| Chemical Name |
4-N,6-N-dicyclopentyl-2-methylsulfanyl-5-nitropyrimidine-4,6-diamine
|
| Synonyms |
GS 39783; GS-39783; GS39783
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~74.09 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9635 mL | 14.8174 mL | 29.6349 mL | |
| 5 mM | 0.5927 mL | 2.9635 mL | 5.9270 mL | |
| 10 mM | 0.2963 mL | 1.4817 mL | 2.9635 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
