2. Anti-infection Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Parasite Reactive Oxygen Species (ROS)
  4. Antileishmanial agent-40

Antileishmanial agent-40 是一种具有口服活性和选择性的抗利什曼原虫剂。Antileishmanial agent-40 可升高杜氏利什曼原虫前鞭毛体内的细胞活性氧 (ROS) 水平。Antileishmanial agent-40 可诱导杜氏利什曼原虫前鞭毛体细胞周期阻滞于 sub-G0/G1 期，提示类程序性寄生虫死亡。Antileishmanial agent-40 可用于利什曼病的研究。

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Antileishmanial agent-40

Antileishmanial agent-40 Chemical Structure

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Antileishmanial agent-40 相关抗体

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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

Antileishmanial agent-40 is an orally active and selective antileishmanial agent. Antileishmanial agent-40 elevates intracellular reactive oxygen species (ROS) levels in Leishmania donovani promastigotes. Antileishmanial agent-40 induces cell cycle arrest at the sub-G0/G1 phase in Leishmania donovani promastigotes, indicative of programmed-like parasite death. Antileishmanial agent-40 can be used for the research of leishmaniasis[1].

IC50 & Target[1]

Leishmania

 

体外研究
(In Vitro)

Antileishmanial agent-40 (Compound 19e) (2-16 μg/mL；48 小时) 对 RAW 264.7 巨噬细胞表现出中等细胞毒性，其 CC50 为 7.56 μg/mL[1]。
Antileishmanial agent-40 (2-16 μg/mL；48 小时) 可强效抑制 Leishmania donovani 前鞭毛体的生长，其 IC50 为 1.86 μg/mL[1]。
Antileishmanial agent-40 (1.86 μg/mL；48 小时) 可在杜氏利什曼原虫前鞭毛体中诱导显著的细胞周期阻滞，有 66.9%的细胞停滞于亚 G0/G1 期[1]。
Antileishmanial agent-40 (1.86 μg/mL；48 小时) 可使杜氏利什曼原虫前鞭毛体的细胞内活性氧水平显著升高 4.72 倍[1]。

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

Antileishmanial agent-40 相关抗体:

Cell Cycle Analysis[1]

Cell Line: Leishmania donovani promastigotes
Concentration: 1.86 μg/mL
Incubation Time: 48 h
Result: Significantly increased the proportion of L. donovani promastigotes in the sub-G0/G1 phase to 66.9% (p < 0.001), compared to 6.8% in untreated parasites and 56.0% in miltefosine-treated parasites.
体内研究
(In Vivo)

Antileishmanial agent-40 (Compound 19e) (0.5-20 mg/kg；口服；单次给药) 在雌性 BALB/c 小鼠中的耐受性良好，单次口服剂量最高可达 20 mg/kg；在最高测试剂量下仅观察到轻微的、处于参考范围内的生化指标变化，未出现死亡或明显毒性[1]。

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

Animal Model: BALB/c (female, 24-25 g, acute oral toxicity model)[1]
Dosage: 0.5 mg/kg; 1 mg/kg; 2 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: p.o.; single dose
Result: Showed no mortality, abnormal behavior, or visible toxicity signs across all dose groups.
Exhibited negligible body weight changes.
Demonstrated no significant hematological alterations compared to controls.
Revealed normal tissue architecture in liver, spleen, and kidney, with only minor, non-significant alterations in the 10 and 20 mg/kg groups.
Caused significantly elevated serum urea (25.97 mg/dl) and creatinine (0.73 mg/dl) compared to controls at 10 mg/kg, with no change in uric acid.
Induced significantly elevated serum urea (26.03 mg/dl), creatinine (0.80 mg/dl), uric acid (5.10 mg/dl), ALT, AST, and ALP levels, plus slightly elevated cholesterol (184.3 mg/dl), triglycerides, HDL, LDL, and VLDL levels compared to controls at 20 mg/kg.
Showed all elevated values remained within reference ranges.
Noted no significant biochemical toxicity at 0.5, 1, 2, or 5 mg/kg.
分子量

431.41

Formula

C22H31BrN4
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

Antileishmanial agent-40 相关分类

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  • 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:

Antileishmanial agent-40Antileishmanial agent40Antileishmanial agent 40ParasiteReactive Oxygen Species (ROS)sub-G0/G1 phaseprogrammed-like parasite deathBALB/c miceRAW 264.7 macrophagesreactive oxygen speciesmammalian cellsleishmaniasisLeishmania donovani promastigotescell cycle arrestInhibitorinhibitorinhibit

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