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  4. WM382

WM382 是一种口服有效的双血浆蛋白酶 IX/X (PMIX/X) 抑制剂，IC50 分别为 1.4 nM 和 0.03 nM。WM382 在疟原虫生命周期的多个阶段具有良好的体内疗效和良好的耐药性。

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WM382 Chemical Structure

WM382 Chemical Structure

CAS No. : 2606990-92-3

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规格 价格 是否有货 数量
1 mg ￥7200
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Customer Review

WM382 相关抗体

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(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].

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

WM382 相关抗体:
体内研究
(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].

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.
分子量

504.62

Formula

C29H36N4O4
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 5 mg/mL (9.91 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.35%

COA (269 KB) HNMR (321 KB) RP-HPLC (435 KB)

产品使用指南 (1538 KB)
参考文献

WM382 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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产品名称：
WM382
目录号：
HY-151561
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