1. Anti-infection Membrane Transporter/Ion Channel
  2. Parasite Na+/K+ ATPase
  3. MMV1581361

MMV1581361 是一种 PfATP4 抑制剂,同时也是一种口服有效的阻断传播剂,对恶性疟原虫血液阶段分离株具有纳摩尔级活性。MMV1581361 会破坏恶性疟原虫体内的钠离子 (Na+) 稳态。MMV1581361 可抑制雄配子出丝、降低卵囊密度,并阻断恶性疟原虫的传播。MMV1581361 在人源化恶性疟原虫 NOD scid IL2Rγnull 小鼠模型中展现出疗效。MMV1581361 可用于疟疾相关研究。

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MMV1581361

MMV1581361 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MMV1581361 is a PfATP4 inhibitor and an orally active, transmission-blocking agent with nanomolar activity against Plasmodium falciparum blood-stage isolates. MMV1581361 disrupts sodium ion (Na+) homeostasis in Plasmodium falciparum. MMV1581361 inhibits male gamete exflagellation, reduces oocyst intensity, and blocks transmission of Plasmodium falciparum. MMV1581361 demonstrates efficacy in the humanized Plasmodium falciparum NOD scid IL2Rγnull mouse model. MMV1581361 can be used for the research of malaria[1].

IC50 & Target[1]

Plasmodium

 

体外研究
(In Vitro)

MMV1581361 (compound 15) 可强效抑制血液期恶性疟原虫 Pf3D7 的生长,其 IC50 为 0.03 μM;同时可抑制 Chloroquine (HY-17589A) 抗性血液期恶性疟原虫 PfDd2 的生长,IC50 为 0.02 μM[1]
MMV1581361 (25 μM; 72 h) 的动力学溶解度为 12.87 μM,在 25 μM 浓度下对 HepG2 细胞无细胞毒性,且在大鼠肝细胞中稳定性高,半衰期为 480 min[1]
MMV1581361 对恶性疟原虫红内期寄生虫表现出中等强度的体外杀伤活性[1]
MMV1581361 (1 μM; 48 h) 对恶性疟原虫表现出强大的传播阻断活性,可抑制 90% 的雄配子出丝,使平均卵囊强度降低 98%,并阻断 88% 的传播[1]
MMV1581361 (1-1000 nM; 1 μM) 可导致恶性疟原虫 Pf3D7 滋养体的胞质 Na+ 浓度呈剂量依赖性升高,且在 Concanavalin A (HY-P2149) 存在的情况下会升高胞质 pH[1]

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

体内研究
(In Vivo)

MMV1581361 (compound 15) (灌胃给药,25 mg/kg,每日 1 次,连续 4 天) 可使源人化 NOD scid IL2Rγnull 小鼠的原虫血症抑制率 > 99.9%,并在感染后第 6 天清除所有显微镜可检测到的恶性疟原虫[1]

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

Animal Model: NOD scid IL2Rγnull (engrafted with human erythrocytes, infected with pf3D70087/N7)[1]
Dosage: 25 mg/kg (once daily for 4 consecutive days)
Administration: p.o.; once daily; 4 consecutive days
Result: Demonstrated a dose- and time-dependent reduction in parasitemia, clearing all microscopy-detectable parasites by day 6 postinfection.
Achieved > 99.9% reduction in parasitemia relative to untreated control mice on day 7 postinfection.
分子量

434.46

Formula

C16H17F3N4O3S2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
MMV1581361
目录号:
HY-181821
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