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  4. 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.

For research use only. We do not sell to patients.

WM382 Chemical Structure

WM382 Chemical Structure

CAS No. : 2606990-92-3

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Based on 1 publication(s) in Google Scholar

WM382 Related Antibodies

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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[1][2][3].

IC50 & Target

Plasmodium

 

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)[2][3].
WM382 selectively binds PMV and PMX with Ki 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 Related Antibodies
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[3].

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

Animal Model: Mice infected with P. berghei[3]
Dosage: 20 mg/kg
Administration: Oral gavage; twice daily for 4 days; monitored for 30 days
Result: Cured mice of P. berghei and prevents blood infection from the liver.
Animal Model: Humanized nonobese diabetic-severe combined immunodeficiency (NOD-scid) IL2Rgnull mouse model (NSG)[3]
Dosage: 1, 3, 10, 30 mg/kg
Administration: Oral gavage; once daily for 4 days; monitored for 7 days
Result: Cleared of parasitemia by day 6 at 30 mg/kg or day 7 at 3 and 10 ma/kg.
Molecular Weight

504.62

Formula

C29H36N4O4
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (9.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9817 mL 9.9084 mL 19.8169 mL
5 mM 0.3963 mL 1.9817 mL 3.9634 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.35%

COA (254 KB) HNMR (321 KB) RP-HPLC (435 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9817 mL 9.9084 mL 19.8169 mL 49.5422 mL
5 mM 0.3963 mL 1.9817 mL 3.9634 mL 9.9084 mL
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WM382 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WM3822606990-92-3WM 382WM-382Parasitemalaria parasitein vivo efficacyantimalarialaspartic proteaseenzzyme kineticsmalariaprotein-drug structureInhibitorinhibitorinhibit

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