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.
WM382 structure
CAS No.: 2606990-92-3
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 4,800.00 | BP-02241-100mg | In stock | Get quote |
| 250 mg | Inquire | BP-02241-250mg | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
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