Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
Plasmodium
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ln Vitro |
WM382 inhibits Plasmodium falciparum and P. vivax, with an IC50 value of 0.6 nM for P. falciparum, and exhibits considerable cytotoxicity against HepG2 cells (IC50=24.8 μM)[2][3]. With Ki values of 13.4 μM and 0.035 nM, respectively, WM382 binds PMV and PMX selectively[3]. The time to patent blood infection after injection is reminded by WM382 (1 nM and 100 nM) in P. berghei-infected HepG2 in vitro cultures[3].
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ln Vivo |
In mouse models of P. berghei and P. falciparum parasites, WM382 (20 mg/kg twice daily or 1-30 mg/kg once day; po; for 4 d) is effective in eliminating infections. Asexual P. falciparum infection in humanized mice can be effectively treated with WM382, which also stops mosquito transmission[3].
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Animal Protocol |
Animal/Disease Models: Mice infected with P. berghei[3]
Doses: 20 mg/kg Route of Administration: po (oral gavage); twice (two times) daily for 4 days; monitored for 30 days Experimental Results: Cured mice of P. berghei and prevents blood infection from the liver. Animal/Disease Models: Humanized nonobese diabetic-severe combined immunodeficiency (NOD-scid) IL2Rgnull mouse model (NSG)[3] Doses: 1, 3, 10, 30 mg/kg Route of Administration: po (oral gavage); one time/day for 4 days; monitored for 7 days Experimental Results: Cleared of parasitemia by day 6 at 30 mg/kg or day 7 at 3 and 10 ma/kg . |
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. |
Molecular Formula |
C29H36N4O4
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Molecular Weight |
504.62
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CAS # |
2606990-92-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1OC2=CC=C(C(N[C@@H]3C4=CC=CC=C4OC(C)(C)C3)=O)C=C2[C@H](N2C(N)=NC(CC)(CC)CC2=O)C1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 5 mg/mL (9.91 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | |
10 mM | 0.1982 mL | 0.9908 mL | 1.9817 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.