2. Anti-infection NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Autophagy
  3. Parasite Reactive Oxygen Species (ROS) Autophagy
  4. Antileishmanial agent-43

Antileishmanial agent-43 is a 3,4,5‑trisubstituted isoxazole with selective antileishmanial activity. Antileishmanial agent-43 shows IC50 values of 12.7 μM against Leishmania amazonensis promastigotes and 0.96 μM against intracellular amastigotes. Antileishmanial agent-43 induces ROS elevation, oxidative stress and mitochondrial dysfunction, resulting in lipid peroxidation, mitochondrial depolarization and ATP imbalance. Antileishmanial agent-43 causes cell shrinkage, phosphatidylserine externalization, plasma membrane permeabilization, and promotes autophagy. Antileishmanial agent-43 can be used for the research of leishmaniasis.

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Antileishmanial agent-43

Antileishmanial agent-43 Chemical Structure

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Antileishmanial agent-43 Related Antibodies

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Description

Antileishmanial agent-43 is a 3,4,5‑trisubstituted isoxazole with selective antileishmanial activity. Antileishmanial agent-43 shows IC50 values of 12.7 μM against Leishmania amazonensis promastigotes and 0.96 μM against intracellular amastigotes. Antileishmanial agent-43 induces ROS elevation, oxidative stress and mitochondrial dysfunction, resulting in lipid peroxidation, mitochondrial depolarization and ATP imbalance. Antileishmanial agent-43 causes cell shrinkage, phosphatidylserine externalization, plasma membrane permeabilization, and promotes autophagy. Antileishmanial agent-43 can be used for the research of leishmaniasis[1].

IC50 & Target[1]

Leishmania

 

In Vitro

Antileishmanial agent-43 (compound 4) (1-100 μM; 72 h) inhibits proliferation of Leishmania amazonensis promastigotes (IC50 = 12.7 μM)[1].
Antileishmanial agent-43 (0.1-100 μM; 48 h) suppresses growth of Leishmania amazonensis intracellular amastigotes (IC50 = 0.96 μM)[1].
Antileishmanial agent-43 (10-1000 μM; 48 h) exhibits low cytotoxicity against J774A.1 macrophages (CC50 = 196.1 μM) and L929 fibroblasts (CC50 = 232.1 μM)[1].
Antileishmanial agent-43 (12.7 μM, 25.4 μM for promastigotes; 0.96 μM, 1.92 μM for amastigotes; 24 h) elevates ROS and nitric oxide levels, induces lipid peroxidation, triggers mitochondrial depolarization, disturbs ATP homeostasis, causes cell shrinkage, phosphatidylserine externalization, plasma membrane permeabilization, and promotes autophagic vacuole and acidic compartment formation in Leishmania amazonensis promastigotes and amastigotes[1].
Antileishmanial agent-43 (12.7 μM, 25.4 μM for promastigotes; 0.96 μM, 1.92 μM for amastigotes; 72 h for promastigotes, 48 h for amastigotes) induces morphological and ultrastructural alterations in Leishmania amazonensis promastigotes and intracellular amastigotes[1].

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

Antileishmanial agent-43 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Leishmania amazonensis promastigotes and intracellular amastigotes
Concentration: 12.7 μM, 25.4 μM (promastigotes); 0.96 μM, 1.92 μM (amastigotes)
Incubation Time: 24 h
Result: Induced apoptosis-like death, including phosphatidylserine externalization, cell shrinkage, and plasma membrane permeabilization in both promastigotes and amastigotes.

Cell Autophagy Assay[1]

Cell Line: Leishmania amazonensis promastigotes and intracellular amastigotes
Concentration: 12.7 μM, 25.4 μM (promastigotes); 0.96 μM, 1.92 μM (amastigotes)
Incubation Time: 24 h
Result: Promoted the formation of autophagic vacuoles and acidic compartments in both promastigotes and amastigotes.

Immunofluorescence[1]

Cell Line: Leishmania amazonensis promastigotes and intracellular amastigotes
Concentration: 12.7 μM, 25.4 μM (promastigotes); 0.96 μM, 1.92 μM (amastigotes)
Incubation Time: 24 h
Result: Detected elevated ROS and nitric oxide levels, as well as mitochondrial depolarization in treated parasites via fluorescence-based methods.
Molecular Weight

460.42

Formula

C23H17FN6O4
SMILES

O=C(C1=NOC(C2=CC=C([N+]([O-])=O)C=C2)=C1CNC3=CC=C(F)C=C3)N/N=C/C4=NC=CC=C4
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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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Antileishmanial agent-43 Related Classifications

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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.

Keywords:

Antileishmanial agent-43Antileishmanial agent43Antileishmanial agent 43ParasiteReactive Oxygen Species (ROS)Autophagynitric oxidemammalian cellslipid peroxidationreactive oxygen specieslipid droplet accumulationoxidative stressapoptosis-like cell deathintracellular amastigotesmitochondrial depolarizationLeishmania amazonensis promastigotesInhibitorinhibitorinhibit

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