WM382 

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^[1][2][3].

WM382 shows moderate cytotoxicity against HepG2 cells (IC₅₀=24.8 μM), and inhibits Plasmodium falciparum and P. vivax with an IC₅₀ value of 0.6 nM (P. falciparum)^[2][3].
WM382 selectively binds PMV and PMX with K_i values of 13.4 μM and 0.035 nM, respectively^[3].
WM382 (1 nM and 100 nM) reminds the time to patent blood infection following injection of 65 h in P. berghei-infected HepG2 in vitro cultures^[3].

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

WM382 (20 mg/kg twice daily or 1-30 mg/kg once daily; p.o.; for 4 d) can clear mouse models of P. berghei and P. falciparum parasites. WM382 is also efficacious against P. falciparum asexual infection in humanized mice and prevents transmission to mosquitoes^[3].

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

504.62

C₂₉H₃₆N₄O₄

2606990-92-3

Solid

White to off-white

O=C(C1=CC([C@H](N(C(NC(CC)(CC)C2)=N)C2=O)CCO3)=C3C=C1)N[C@H]4CC(C)(C)OC5=C4C=CC=C5

Room temperature in continental US; may vary elsewhere.

* 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.

• [1]. Manuel de LR, et al. The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria. ACS Med Chem Lett. 2022 Oct 12.

  [2]. Hodder AN, et al. Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax. Structure. 2022 Jul 7;30(7):947-961.e6.  [Content Brief]

  [3]. Favuzza P, et al. Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle. Cell Host Microbe. 2020 Apr 8;27(4):642-658.e12.  [Content Brief]