GSK369796 Dihydrochloride
Based on 1 Customer Validation
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.
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- Pureté: 99.56%
- CAS No.: 1010411-21-8
- Formule: C20H24Cl3N3O
- Masse moléculaire:428.78
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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Plasmodium |
In Vitro
In vitro, GSK369796 Dihydrochloride can inhibit the growth of Plasmodium falciparum strains 3D7c, HB3c and K1d, with IC50s of 11.2±2.2, 12.6±5.3 and 13.2±3.2 nM, respectively. Protein binding is higher for GSK369796 Dihydrochloride (compound 4) compare to desethyl amodiaquine in the mouse (93 vs 74%) but similar in human (88 vs 86%). GSK369796 Dihydrochloride can also inhibit hERG potassium ion channel repolarization with an IC50 of 7.5±0.8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1010411-21-8
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Appearance Solid
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Masse moléculaire 428.78
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Formule C20H24Cl3N3O
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Color Light yellow to yellow
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SMILES
OC1=CC(NC2=CC=NC3=CC(Cl)=CC=C23)=CC=C1CNC(C)(C)C.[H]Cl.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (233.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (116.61 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.5 mg/mL (5.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocole
Cell Assay[1]
Assays are performed in sterile 96-well microtiter plates, each plate contains 200 mL of parasite culture (2% parasitemia, 0.5% hematocrit) with or without 10 mL drug dilutions (including GSK369796 Dihydrochloride). Each drug is tested in triplicate and parasite growth is compared to control wells (which constitutes 100% parasite growth). Cultures are incubated for a further 24 h before they are harvested onto filter mats, dried for 1 h at 55 °C, and counted. IC50 values are calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
The efficacy of selected 4-aminoquinolines (including GSK369796 Dihydrochloride) is measured against P. yoelii or P. berghei in a 4-day test. 28 Cohorts of age-matched female mice are infected iv with 6.4×106 or 10.0×106 parasites obtained from infected donors, and the mice are randomly distributed in groups of n=5 mice/group (day 0). Treatments are administered from day 0 (one hour after infection) until day 3. The therapeutic efficacy of compounds (including GSK369796 Dihydrochloride) is expressed as the effective dose that reduces parasitemia by 50% (ED50) and 90% (ED90) with respect to vehicle treated groups (ED90) and the dose that achieved eradication of parasitemia until day 23 after infection (NRL). All compounds (including GSK369796 Dihydrochloride) and corresponding vehicles are administered orally at 20 mg/kg or subcutaneously at 10 mg/kg, as appropriate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3322 mL | 11.6610 mL | 23.3220 mL | 58.3050 mL |
| 5 mM | 0.4664 mL | 2.3322 mL | 4.6644 mL | 11.6610 mL | |
| 10 mM | 0.2332 mL | 1.1661 mL | 2.3322 mL | 5.8305 mL | |
| 15 mM | 0.1555 mL | 0.7774 mL | 1.5548 mL | 3.8870 mL | |
| 20 mM | 0.1166 mL | 0.5830 mL | 1.1661 mL | 2.9152 mL | |
| 25 mM | 0.0933 mL | 0.4664 mL | 0.9329 mL | 2.3322 mL | |
| 30 mM | 0.0777 mL | 0.3887 mL | 0.7774 mL | 1.9435 mL | |
| 40 mM | 0.0583 mL | 0.2915 mL | 0.5830 mL | 1.4576 mL | |
| 50 mM | 0.0466 mL | 0.2332 mL | 0.4664 mL | 1.1661 mL | |
| 60 mM | 0.0389 mL | 0.1943 mL | 0.3887 mL | 0.9717 mL | |
| 80 mM | 0.0292 mL | 0.1458 mL | 0.2915 mL | 0.7288 mL | |
| 100 mM | 0.0233 mL | 0.1166 mL | 0.2332 mL | 0.5830 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
GSK369796 Dihydrochloride Related Classifications
HY-12082A Related Classifications
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