WM382 free base · Synonyms: WM-382 · WM 382

WM382 is an orally active and potent dual plasmepsin IX/X inhibitor.

For research use only. Not for human or veterinary use.

Target Parasite

Research area Infection

Purity >98% Stock Inquire

Data Sheet SDS COA

WM382 structure

CAS No.: 2606990-92-3

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Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 765.00	BP-02241-50mg	In stock	Get quote
100 mg	USD 969.00	BP-02241-100mg	In stock	Get quote
250 mg	USD 1,676.00	BP-02241-250mg	In stock	Get quote
500 mg	USD 2,860.00	BP-02241-500mg	In stock	Get quote
1 g	Inquire	BP-02241-1g	In stock	Inquire

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Description

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.

Biological activity

In Vitro 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). WM382 selectively binds PMV and PMX with Ki values of 13.4 μM and 0.035 nM, respectively. 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. In Vivo 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.

Identifiers

SMILES: 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
InChIKey: ZSZSSSHEMYULPX-FCHUYYIVSA-N

Specifications

MW (average): 504.6205
Formula: C₂₉H₃₆N₄O₄
CAS No.: 2606990-92-3
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO 5 mg/mL

Documents

References

[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.

[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.

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