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

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.

For research use only. We do not sell to patients.

Antileishmanial agent-40

Antileishmanial agent-40 Chemical Structure

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Description

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

 

In Vitro

Antileishmanial agent-40 (Compound 19e) (2-16 μg/mL; 48 h) exhibits moderate cytotoxicity toward RAW 264.7 macrophages with a CC50 of 7.56 μg/mL[1].
Antileishmanial agent-40 (2-16 μg/mL; 48 h) potently inhibits Leishmania donovani promastigote growth with an IC50 of 1.86 μg/mL[1].
Antileishmanial agent-40 (1.86 μg/mL; 48 h) induces pronounced cell cycle arrest in Leishmania donovani promastigotes, with 66.9% of cells accumulating in the sub-G0/G1 phase[1].
Antileishmanial agent-40 (1.86 μg/mL; 48 h) induces a significant 4.72-fold increase in intracellular reactive oxygen species levels in Leishmania donovani promastigotes[1].

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

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.
In Vivo

Antileishmanial agent-40 (Compound 19e) (0.5-20 mg/kg; p.o.; single dose) is well tolerated in female BALB/c mice up to a single oral dose of 20 mg/kg, with only mild, within-reference-range biochemical alterations observed at the highest tested doses and no mortality or overt toxicity[1].

MedChemExpress (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.
Molecular Weight

431.41

Formula

C22H31BrN4

SMILES

CCCCC1=NN2C(C3=CC=C(Br)C=C3N=C2NC(C)(C)CC(C)(C)C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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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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Antileishmanial agent-40
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HY-183262
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