| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
MMV390048 targets Plasmodium phosphatidylinositol 4-kinase (PI4K), an enzyme essential for the parasite's intracellular life cycle. By inhibiting PI4K, MMV390048 disrupts the parasite's ability to replicate and survive within host cells.
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| ln Vitro |
With IC50 and IC90 values of 28 and 40 nM, respectively, MMV390048 displays a steep inhibition curve against the intraerythrocytic life cycle stage of Plasmodium falciparum (NF54 drug-sensitive strain).
In vitro, MMV390048 potently inhibits P. vivax PI4K with an IC50 of 3.4 nM and is active against P. falciparum with an IC50 of 28 nM. It targets the erythrocytic stage of the P. falciparum life cycle. |
| ln Vivo |
In vivo, MMV390048 decreases the blood levels of P. falciparum in preclinical models. It has shown promising results in preclinical studies and is currently being evaluated in clinical trials.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for MMV390048 involves measuring the kinase activity of Plasmodium PI4K in the presence of the compound. The assay uses ATP and a peptide substrate, and phosphorylation is quantified using a radiometric or fluorescence-based method. The IC50 is determined.
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| Cell Assay |
Cellular assays for MMV390048 involve testing its anti-malarial activity against P. falciparum cultures. The parasite growth inhibition is measured by assessing the incorporation of [3H]hypoxanthine or by using a fluorescence-based assay. The IC50 is determined.
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| Animal Protocol |
In vivo efficacy of MMV390048 is evaluated in mouse models of malaria infection. Mice are infected with P. falciparum or P. berghei, and the compound is administered orally. Parasitemia is monitored by blood smear microscopy, and the reduction in parasite load is measured.
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| ADME/Pharmacokinetics |
MMV390048 has shown favorable pharmacokinetic properties in preclinical studies, supporting its clinical development. It has a molecular weight of 393.38 g/mol and a molecular formula of C18H14F3N3O2S.
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| Toxicity/Toxicokinetics |
Toxicity data for MMV390048 are limited but have been evaluated in preclinical safety studies. No significant toxicity has been reported at therapeutic doses.
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| References | |
| Additional Infomation |
MMV390048 is an investigational antimalarial drug currently in clinical trials. It has not yet received regulatory approval. Its mechanism involves inhibition of Plasmodium PI4K, disrupting the parasite's life cycle.
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| Molecular Formula |
C18H14F3N3O2S
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|---|---|
| Molecular Weight |
393.3842
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| Exact Mass |
393.075
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| CAS # |
1314883-11-8
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| PubChem CID |
53311393
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
534.4±50.0 °C at 760 mmHg
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| Flash Point |
277.0±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
3.06
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
600
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RTJQABCNNLMCJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14F3N3O2S/c1-27(25,26)14-5-2-11(3-6-14)13-8-15(17(22)24-10-13)12-4-7-16(23-9-12)18(19,20)21/h2-10H,1H3,(H2,22,24)
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| Chemical Name |
5-(4-methylsulfonylphenyl)-3-[6-(trifluoromethyl)pyridin-3-yl]pyridin-2-amine
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| Synonyms |
MMV 390048; MMV-390048; MMV390048
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~254.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5421 mL | 12.7104 mL | 25.4207 mL | |
| 5 mM | 0.5084 mL | 2.5421 mL | 5.0841 mL | |
| 10 mM | 0.2542 mL | 1.2710 mL | 2.5421 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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