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WM382 

Cat. No. M29727
WM382  Structure
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Quality Control & Documentation
Biological Activity

WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile.

Chemical Information
Molecular Weight 504.62
Formula C29H36N4O4
CAS Number 2606990-92-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Paola Favuzza, et al. Cell Host Microbe. Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle

[2] Ransford Oduro Kumi, et al. Molecules. Bridging the Gap in Malaria Parasite Resistance, Current Interventions, and the Way Forward from in Silico Perspective: A Review

[3] Manuel de Lera Ruiz, et al. ACS Med Chem Lett. The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria

[4] Anthony N Hodder, et al. Structure. Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax

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  Catalog
Abmole Inhibitor Catalog




Keywords: WM382  supplier, Parasite, inhibitors, activators


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