GSK598809
Based on 1 publication(s) in Google Scholar
GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.73%
- CAS. Nr.: 863680-45-9
- Formel: C22H23F4N5OS
- Molecular Weight:481.51
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Lösungsmittel & Löslichkeit
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- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) GSK598809
MoreAlle Dopamine Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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D3 Receptor |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 863680-45-9
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Appearance Solid
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Molecular Weight 481.51
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Formel C22H23F4N5OS
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Color White to off-white
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SMILES
CC1=C(C2=NN=C(SCCCN3CC4(C5=CC=C(C(F)(F)F)C=C5F)CC4C3)N2C)OC=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Br J Cancer
DRD4 promotes chemo-resistance and cancer stem cell-like phenotypes by mediating the activation of the Akt/β-catenin signaling axis in liver cancer. [Abstract]2024 Oct;131(7):1212-1223. PMID: 39174739
Lösungsmittel & Löslichkeit
DMSO : 83.33 mg/mL (173.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
1M HCl : 28.57 mg/mL (59.33 mM; ultrasonic and adjust pH to 2 with HCl)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Dogs[1]
Male beagle dogs are used throughout the study. The experiment is conducted in phases. In the first (hemodynamics) phase, the dogs are dosed at weekly intervals over a period of 9 weeks with combinations of either GSK598809 or vehicle, followed by either cocaine or vehicle. After the baseline measurements are recorded, technical staff briefly returns to the animal room to administer GSK598809 (or vehicle) to all the dogs via oral gavage and activate the timers on the preloaded and preprogrammed infusion pumps[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Appel NM, et al. Dopamine D3 Receptor Antagonist (GSK598809) Potentiates the Hypertensive Effects of Cocaine in Conscious, Freely-Moving Dogs. J Pharmacol Exp Ther. 2015 Sep;354(3):484-92. [Content Brief]
[2]. Micheli F, et al. 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists. J Med Chem. 2010 Jan 14;53(1):374-91. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 1M HCl / DMSO | 1 mM | 2.0768 mL | 10.3840 mL | 20.7680 mL | 51.9200 mL |
| 5 mM | 0.4154 mL | 2.0768 mL | 4.1536 mL | 10.3840 mL | |
| 10 mM | 0.2077 mL | 1.0384 mL | 2.0768 mL | 5.1920 mL | |
| 15 mM | 0.1385 mL | 0.6923 mL | 1.3845 mL | 3.4613 mL | |
| 20 mM | 0.1038 mL | 0.5192 mL | 1.0384 mL | 2.5960 mL | |
| 25 mM | 0.0831 mL | 0.4154 mL | 0.8307 mL | 2.0768 mL | |
| 30 mM | 0.0692 mL | 0.3461 mL | 0.6923 mL | 1.7307 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5192 mL | 1.2980 mL | |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4154 mL | 1.0384 mL | |
| DMSO | 60 mM | 0.0346 mL | 0.1731 mL | 0.3461 mL | 0.8653 mL |
| 80 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6490 mL | |
| 100 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.5192 mL |
GSK598809 Related Classifications
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