MMV009085
Based on 1 Customer Validation
MMV009085 is a potent PfHT1 (Plasmodium falciparum hexose transporter)-specific inhibitor and a potential anti-malarial agent . MMV009085 is also a human glucose transporter inhibitor, it has high potency in inhibiting both glucose uptake (IC50: 2.6 μM in glucose uptake assay) and growth of the parasites (EC50: 1.23±0.04 μM against 3D7).
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- Purity: 98.68%
- CAS No.: 298217-59-1
- 화학식: C22H22N2O6
- 분자량:410.42
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
4.38 μM
Compound: GNF-Pf-3184
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
MMV009085 inhibits the transport activity of PfHT-1 with an IC50 of 212 ± 39 μM, the EC50 values of MMV009085 in the parasite growth inhibition assay are 1.23 ± 0.04 μM against 3D7 and 0.720 ± 0.05 μM against Dd2. MMV009085 displays significant cytotoxicity with CC50 values of 2.46 ± 0.03 μM and 1.92 ± 0.85 μM for HEK293T and HepG2 cells, respectively[1]. MMV009085 shows IC50 of 2.6 μM in glucose uptake assay in freed parasites, MMV009085 shows an EC50 of 0.987 μM for inhibition of growth of P. falciparum strain 3D7 in in vitro growth inhibition assay, this compound acts through PfHT blockage to inhibit parasite growth ( EC50=0.795 μM).[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 298217-59-1
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Appearance Solid
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분자량 410.42
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화학식 C22H22N2O6
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Color Off-white to pink
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SMILES
O=C1C2=CC=C3C(N(CCCCO)C(C4=CC=C(C2=C34)C(N1CCCCO)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : ≥ 100 mg/mL (243.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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: ≥ 10 mg/mL (24.37 mM); Suspended solution
This protocol yields a suspended solution of ≥ 10 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.
순도&문서
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Data Sheet (282 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)
References
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4365 mL | 12.1826 mL | 24.3653 mL | 60.9132 mL |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL | 12.1826 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4365 mL | 6.0913 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 4.0609 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2183 mL | 3.0457 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4365 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0304 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6091 mL |
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