| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target is the dopamine D3 receptor (DRD3), a G-protein-coupled receptor that is highly expressed in limbic brain regions. (-)-GSK598809 is a selective D3 receptor antagonist that blocks dopamine binding and downstream signaling. It shows high selectivity for D3 over D2 receptors. It may also modulate D3 receptor-mediated behaviors.
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|---|---|
| ln Vitro |
(-)-GSK598809 is a selective dopamine D3 receptor antagonist. It binds to DRD3 with high affinity and blocks dopamine-induced signaling. It shows selectivity for D3 over D2 receptors. It is used as a research tool to study D3 receptor function in addiction and cognition.
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| ln Vivo |
In vivo, (-)-GSK598809 is studied in animal models of addiction, cognition, and psychiatric disorders. It blocks D3 receptor-mediated behaviors. It may potentiate the hypertensive effects of other drugs. Typical doses range from 1-30 mg/kg administered orally or intraperitoneally.
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| Enzyme Assay |
Non-cell assays for (-)-GSK598809 include radioligand binding assays using membranes from cells expressing recombinant human D3 receptor. The assay employs a radiolabeled D3 antagonist such as [3H]spiperone or [125I]iodosulpride. The compound is incubated with membranes and tracer in assay buffer for 60-90 min at 25°C.
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| Cell Assay |
Functional assays use D3 receptor-expressing cells (CHO-K1 or HEK293) and measure inhibition of forskolin-stimulated cAMP accumulation. Cells are treated with the compound and forskolin. cAMP levels are quantified using a competitive immunoassay.
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| Animal Protocol |
In vivo, (-)-GSK598809 is tested in rodent models of addiction and cognition. A typical protocol involves oral administration (1-30 mg/kg) in rats or mice. Drug-seeking behavior is assessed in self-administration models. Cognitive function is assessed using novel object recognition or Morris water maze.
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| References |
| Molecular Formula |
C22H23F4N5OS
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|---|---|
| Molecular Weight |
481.509536981583
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| Exact Mass |
495.17
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| Elemental Analysis |
C, 55.75; H, 5.09; F, 15.34; N, 14.13; O, 3.23; S, 6.47
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| CAS # |
863680-46-0
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| Related CAS # |
GSK598809;863680-45-9; (-)-GSK598809 hydrochloride;863766-31-8; 863680-46-0; 1310803-30-5; 1008521-08-1 (tartrate); 1008521-09-2 (tartrate hydrate)
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| PubChem CID |
11784937
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| Appearance |
Solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
704
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=C(OC=N1)C2=NN=C(N2C)SCCCN3C[C@@H]4C[C@@]4(C3)C5=C(C=C(C=C5)C(F)(F)F)F
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| InChi Key |
ZKRWPAYTJMRKLJ-BTYIYWSLSA-N
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| InChi Code |
InChI=1S/C22H23F4N5OS/c1-13-18(32-12-27-13)19-28-29-20(30(19)2)33-7-3-6-31-10-15-9-21(15,11-31)16-5-4-14(8-17(16)23)22(24,25)26/h4-5,8,12,15H,3,6-7,9-11H2,1-2H3/t15-,21-/m0/s1
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| Chemical Name |
5-[5-[3-[(1S,5R)-1-[2-fluoro-4-(trifluoromethyl)phenyl]-3-azabicyclo[3.1.0]hexan-3-yl]propylsulfanyl]-4-methyl-1,2,4-triazol-3-yl]-4-methyl-1,3-oxazole
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| Synonyms |
(1S,5R)-GSK598809; (-)-GSK-598809; GSK598809; GSK 598809;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0768 mL | 10.3840 mL | 20.7680 mL | |
| 5 mM | 0.4154 mL | 2.0768 mL | 4.1536 mL | |
| 10 mM | 0.2077 mL | 1.0384 mL | 2.0768 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.
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