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Art. -Nr.: HY-182685

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MMV693183

MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC₅₀ of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor.

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CAS. Nr.: 2446681-27-0
Formel: C₁₆H₂₁F₃N₂O₄
Molecular Weight:362.34

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

MMV693183 Chemical Structure

CAS. Nr.: 2446681-27-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Bioz

Biologische Aktivität

Beschreibung

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In Vitro

MMV693183 potently inhibits the in vitro asexual blood-stage growth of Plasmodium falciparum strains with an IC₅₀ of 2.1-2.8 nM; it also inhibits the in vitro growth/schizont maturation of clinical isolates of Plasmodium falciparum and P. vivax with low nanomolar activity^[1].
MMV693183 inhibits the viability of Plasmodium falciparum NF54-HGL gametocytes, with an IC₅₀ of 17.8-38.8 nM at 72 h. MMV693183 also potently inhibits female gametocyte activation (IC₅₀=12 nM), but shows weak activity against male gametogenesis (IC₅₀=1 μM)^[1].
MMV693183 (1.5 nM, 500 nM; 72 h) renders AcAS conditional knockdown Plasmodium falciparum parasites 5-fold hypersensitive under AcAS knockdown conditions^[1].
MMV693183 (10 μM) exhibits no in vitro cytotoxicity in human hepatocytes or HepG2 cells, and shows no significant off-target activity against human receptors, enzymes or channels at the concentration of 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:

Human hepatocytes or HepG2 cells
Concentration:

10 µM
Incubation Time:

72 h
Result:

Exhibited no in vitro cytotoxicity in human hepatocytes or HepG2 cells.

Parmacokinetics

Species	Dose	Route	CL_total	T_1/2	Bioavailability
Mice^[1]	3 mg/kg	i.v.	13.4 mL/min/kg	1.2 h	/
Rat^[1]	3 mg/kg	i.v.	21.1 mL/min/kg	3.1 h	/
Dog^[1]	1 mg/kg	i.v.	11.5 mL/min/kg	4.2 h	/
Rat^[1]	30 mg/kg	p.o.	/	/	121 %
Dog^[1]	2 mg/kg	p.o.	/	/	64 %

In Vivo

MMV693183 (50 mg/kg; p.o.; single dose) reduces P. falciparum parasitemia below detectable levels in humanized NSG mice within three days^[1].
MMV693183 clears P. falciparum parasitemia to undetectable levels in humanized NSG mice within 4-6 days, with a modeled MIC of 3.2 ng/mL and MPC₉₀ of 38.4 ng/mL^[1].
MMV693183 (10-50 mg/kg; daily; 4 days) does not cause hemolytic toxicity in G6PD-A-deficient human erythrocyte-engrafted NSG mice^[1].
MMV693183 (10-1000 mg/kg; p.o.; daily; 3-8 days) is well tolerated in Wistar Han rats at doses up to 1000 mg/kg for 3 days, with a >30-fold exposure safety margin at 30 mg/kg/day relative to predicted human efficacious exposure^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NSG (female, humanized with G6PD-A-deficient human erythrocytes to achieve >60% human erythrocytes)^[1]
Dosage:

10 mg/kg; 25 mg/kg; 50 mg/kg
Administration:

daily; 4 days
Result:

Showed no signs of hemolytic toxicity; did not induce hemolysis of G6PD-A-deficient human erythrocytes.

Chemical Information

CAS. Nr. 2446681-27-0
Molecular Weight 362.34
Formel C₁₆H₂₁F₃N₂O₄
SMILES

OCC(C)(C)[C@@H](O)C(NC[C@H](C)NC(C1=C(C=C(C(F)=C1)F)F)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. de Vries LE, et al. Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183. Nat Commun. 2022;13(1):2158. Published 2022 Apr 20. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
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MMV693183

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Biologische Aktivität

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MMV693183 Related Classifications

HY-182685 Related Classifications