MMV688533
Based on 1 Customer Validation
MMV688533 is an antimalarial agent. MMV688533 interferes with intracellular trafficking, lipid utilization, and endocytosis pathways in Plasmodium falciparum. MMV688533 rapidly kills asexual blood-stage Plasmodium falciparum and Plasmodium vivax parasites in vitro and reduces parasitemia in a Plasmodium falciparum NSG mouse model. MMV688533 can be used for the research of malaria.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.50%
- No. CAS: 2260904-47-8
- Fòrmula: C24H15F6N5O2
- Peso molecular:519.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Plasmodium falciparum sporozoites |
MMV688533 (72 hours) potently inhibits the growth of multiple drug-sensitive and drug-resistant Plasmodium falciparum asexual blood-stage strains in vitro with low nanomolar IC50 values[1].
MMV688533 (72 hours) potently inhibits the growth of ex vivo Plasmodium falciparum clinical isolates from Ugandan patients with a median IC50 of 1.3 nM[1].
MMV688533 (35 to 56 hours) potently inhibits the growth of ex vivo Plasmodium falciparum and Plasmodium vivax clinical isolates from Papua Indonesia with median IC50 values of 18.9 nM and 12.0 nM, respectively[1].
MMV688533 (120 hours total, with daily drug renewal) rapidly kills Plasmodium falciparum 3D7A asexual blood-stage parasites in vitro, achieving a log10 PRR of nearly 5 over 48 hours at 10× IC50, with a 24-hour killing rate comparable to dihydroartemisinin[1].
MMV688533 (120 hours total) rapidly reduces viable Plasmodium falciparum asexual blood-stage parasite count[1].
MMV688533 (72 hours) has low-grade resistance conferred by PfACG1 mutations in Plasmodium falciparum 3D7-A10 parasites in vitro, while the PfEHDD218Y mutation enhances resistance only when combined with the PfACG1G98V mutation[1].
MMV688533 shows minimal cytotoxicity against mammalian cells in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (female, 23-28 g, humanized with ≥40% human erythrocytes, infected with Plasmodium falciparum Pf3D70087/N9)[1]
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Dosage:0.5 mg/kg; 1 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg; 50 mg/kg; 75 mg/kg
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Administration:p.o.; single dose
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Result:Reduced parasitemia to below the limit of detection within 48 hours with a single oral dose of 5 mg/kg, followed by recrudescence to 1% by day 18.
Calculated the 90% effective dose (ED90) as 2 mg/kg, corresponding to the single dose required to reduce parasitemia by >90% by day 7 compared to vehicle-treated mice.
Produced >90% reduction in parasitemia by day 7 with four consecutive daily doses of 0.9 mg/kg.
Cleared parasites as rapidly as dihydroartemisinin (50 mg/kg) with single doses of at least 5 mg/kg.
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Animal Model:NSG (female, 23-28 g, humanized with ≥40% human erythrocytes, infected with Plasmodium falciparum Pf3D70087/N9)[1]
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Dosage:0.9 mg/kg
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Administration:p.o.; daily for 4 consecutive days
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Result:Produced >90% reduction in parasitemia by day 7.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2260904-47-8
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Appearance Solid
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Peso molecular 519.40
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Fòrmula C24H15F6N5O2
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Color White to off-white
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SMILES
O=C(C1=CC(C#CC2=CC=C(C(F)(F)F)C(C(NC3=NC=CC=C3)=O)=C2)=CC(C(F)(F)F)=C1)NC(N)=N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (192.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 5 mg/mL (9.63 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Murithi JM, et al. The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance. Sci Transl Med. 2021 Jul 21;13(603):eabg6013. [Content Brief]
[2]. Kavthe RD, et al. A sustainable, efficient, and potentially cost-effective approach to the antimalarial drug candidate MMV688533. Chem Sci. 2023;14(23):6399-6407. Published 2023 May 26. [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, 6 months; -20°C, 1 month. 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 |
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| DMSO | 1 mM | 1.9253 mL | 9.6265 mL | 19.2530 mL | 48.1325 mL |
| 5 mM | 0.3851 mL | 1.9253 mL | 3.8506 mL | 9.6265 mL | |
| 10 mM | 0.1925 mL | 0.9626 mL | 1.9253 mL | 4.8132 mL | |
| 15 mM | 0.1284 mL | 0.6418 mL | 1.2835 mL | 3.2088 mL | |
| 20 mM | 0.0963 mL | 0.4813 mL | 0.9626 mL | 2.4066 mL | |
| 25 mM | 0.0770 mL | 0.3851 mL | 0.7701 mL | 1.9253 mL | |
| 30 mM | 0.0642 mL | 0.3209 mL | 0.6418 mL | 1.6044 mL | |
| 40 mM | 0.0481 mL | 0.2407 mL | 0.4813 mL | 1.2033 mL | |
| 50 mM | 0.0385 mL | 0.1925 mL | 0.3851 mL | 0.9626 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3209 mL | 0.8022 mL | |
| 80 mM | 0.0241 mL | 0.1203 mL | 0.2407 mL | 0.6017 mL | |
| 100 mM | 0.0193 mL | 0.0963 mL | 0.1925 mL | 0.4813 mL |
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