MMV1581361
MMV1581361 is a PfATP4 inhibitor and an orally active, transmission-blocking agent with nanomolar activity against Plasmodium falciparum blood-stage isolates. MMV1581361 disrupts sodium ion (Na+) homeostasis in Plasmodium falciparum. MMV1581361 inhibits male gamete exflagellation, reduces oocyst intensity, and blocks transmission of Plasmodium falciparum. MMV1581361 demonstrates efficacy in the humanized Plasmodium falciparum NOD scid IL2Rγnull mouse model. MMV1581361 can be used for the research of malaria.
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- Formule: C16H17F3N4O3S2
- Masse moléculaire:434.46
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Plasmodium |
MMV1581361 (compound 15) potently inhibits the growth of Plasmodium falciparum Pf3D7 blood-stage parasites with an IC50 of 0.03 μM and inhibits the growth of Chloroquine (HY-17589A) -resistant Plasmodium falciparum PfDd2 blood-stage parasites with an IC50 of 0.02 μM[1].
MMV1581361 (25 μM; 72 h) has a kinetic solubility of 12.87 μM, is noncytotoxic to HepG2 cells at 25 μM, and exhibits high stability in rat hepatocytes with a half-life of 480 min[1].
MMV1581361 exerts a moderate in vitro killing profile against Plasmodium falciparum blood-stage parasites[1].
MMV1581361 (1 μM; 48 h) exhibits strong transmission-blocking activity against Plasmodium falciparum, inhibiting male gamete exflagellation by 90%, reducing mean oocyst intensity by 98%, and blocking transmission by 88%[1].
MMV1581361 (1-1000 nM; 1 μM) causes a dose-dependent increase in cytosolic Na+ concentration in Plasmodium falciparum 3D7 trophozoites and increasing cytosolic pH in the presence of Concanavalin A (HY-P2149)[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:NOD scid IL2Rγnull (engrafted with human erythrocytes, infected with pf3D70087/N7)[1]
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Dosage:25 mg/kg (once daily for 4 consecutive days)
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Administration:p.o.; once daily; 4 consecutive days
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Result:Demonstrated a dose- and time-dependent reduction in parasitemia, clearing all microscopy-detectable parasites by day 6 postinfection.
Achieved > 99.9% reduction in parasitemia relative to untreated control mice on day 7 postinfection.
Chemical Information
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Masse moléculaire 434.46
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Formule C16H17F3N4O3S2
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SMILES
CNC(C1=CC(S(N(CC2)CCN2C3=CC=C(C(F)(F)F)C=N3)(=O)=O)=CS1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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