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.
For research use only. We do not sell to patients.
- Formula: C23H17FN6O4
- Molecular Weight:460.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
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Leishmania |
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.
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Cell Line:Leishmania amazonensis promastigotes and intracellular amastigotes
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Concentration:12.7 μM, 25.4 μM (promastigotes); 0.96 μM, 1.92 μM (amastigotes)
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Incubation Time:24 h
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Result:Induced apoptosis-like death, including phosphatidylserine externalization, cell shrinkage, and plasma membrane permeabilization in both promastigotes and amastigotes.
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Cell Line:Leishmania amazonensis promastigotes and intracellular amastigotes
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Concentration:12.7 μM, 25.4 μM (promastigotes); 0.96 μM, 1.92 μM (amastigotes)
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Incubation Time:24 h
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Result:Promoted the formation of autophagic vacuoles and acidic compartments in both promastigotes and amastigotes.
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Cell Line:Leishmania amazonensis promastigotes and intracellular amastigotes
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Concentration:12.7 μM, 25.4 μM (promastigotes); 0.96 μM, 1.92 μM (amastigotes)
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Incubation Time:24 h
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Result:Detected elevated ROS and nitric oxide levels, as well as mitochondrial depolarization in treated parasites via fluorescence-based methods.
Chemical Information
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Molecular Weight 460.42
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Formula C23H17FN6O4
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antileishmanial agent-43
- Antileishmanial agent43
- Antileishmanial agent 43
- Parasite
- Reactive Oxygen Species (ROS)
- Autophagy
- nitric oxide
- mammalian cells
- lipid peroxidation
- reactive oxygen species
- lipid droplet accumulation
- oxidative stress
- apoptosis-like cell death
- intracellular amastigotes
- mitochondrial depolarization
- Leishmania amazonensis promastigotes
- Inhibitor
- inhibitor
- inhibit