WM382
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2606990-92-3
- 分子式: C29H36N4O4
- 分子量:504.62
-
保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Parasite アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
|
Plasmodium |
体外実験
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. .
体内実験
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.
化学情報
-
CAS 番号 2606990-92-3
-
性状 Solid
-
分子量 504.62
-
分子式 C29H36N4O4
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (278 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[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]
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 |
WM382 関連分類
HY-151561 関連分類
Powered by Bioz