Antileishmanial agent-44
Antileishmanial agent-44 is a histone deacetylase inhibitor targeting Leishmania donovani Sir2, with an IC50 of 0.652 μM against amastigotes. Antileishmanial agent-44 elevates ROS levels to induce oxidative stress, which causes mitochondrial membrane potential depolarization, cytochrome c release, phosphatidylserine externalization and DNA fragmentation, triggers apoptosis-like cell death, and arrests the cell cycle. Antileishmanial agent-44 upregulates the expression of Th1-type cytokines and NO in macrophages, reshapes host immune responses to eliminate intracellular parasites. Antileishmanial agent-44 inhibits parasites in infected golden hamsters in vivo. Antileishmanial agent-44 can be used for the research of visceral leishmaniasis.
For research use only. We do not sell to patients.
- Formula: C30H28N4
- Molecular Weight:444.57
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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 0.652 μM (IC50) |
TNF-α |
IL-10 |
Antileishmanial agent-44 (11ad) potently inhibits Leishmania donovani amastigotes in J774A.1 macrophages, with an IC50 of 0.652 μM, and achieves an inhibition rate of 99% after treatment at 25 μM for 72 h[1].
Antileishmanial agent-44 exhibits low cytotoxicity against J774A.1 macrophages, with a CC50 of 529.0 μM and a selectivity index of 811.3[1].
Antileishmanial agent-44 (48 h) regulates host immune responses in Leishmania donovani-infected J774A.1 macrophages by upregulating the Th1 cytokines TNF-α and IFN-γ, and downregulating the Th2 cytokine IL-10[1].
Antileishmanial agent-44 (10 μM; 24-48 h) induces nitric oxide production in J774A.1 macrophages; after treatment with 10 μM for 24 h and 48 h, 39.1% and 62.4% of the cells exhibit nitric oxide-related fluorescence, respectively[1].
Antileishmanial agent-44 (10 μM; 60-90 min) potently inhibits the histone deacetylase activity of purified recombinant Leishmania donovani Sir2 protein, reaching an inhibition rate of 77.83% at 10 μM after 60−90 min of incubation[1].
Antileishmanial agent-44 (10-50 μM; 24-72 h) induces apoptosis-like cell death in Leishmania donovani promastigotes; significant oligonucleosomal DNA fragmentation is observed after treatment with 50 μM for 48 h and 72 h[1].
Antileishmanial agent-44 (10 μM; 24-48 h) disrupts the cell cycle of Leishmania donovani promastigotes, causing time-dependent accumulation of cells in the sub-G0/G1 phase after treatment at 10 μM[1].
Antileishmanial agent-44 (10 μM; 12-48 h) induces oxidative stress and mitochondrial dysfunction in Leishmania donovani promastigotes, leading to elevated reactive oxygen species (ROS) levels, loss of mitochondrial membrane potential, and time-dependent release of cytochrome c from mitochondria to the cytosol after treatment with 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Leishmania donovani promastigotes
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Concentration:10 μM
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Incubation Time:24, 48 h
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Result:Induced apoptosis-like cell death in Leishmania donovani promastigotes, with ~26.78% and ~29.51% apoptotic cells after 24 h and 48 h of treatment with 10 μM.
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Cell Line:Leishmania donovani promastigotes
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Concentration:10 μM
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Incubation Time:24, 48 h
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Result:Disrupted the cell cycle of Leishmania donovani promastigotes, causing time-dependent accumulation of cells in the sub-G0/G1 phase (6.97% at 24 h, 9.05% at 48 h).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mesocricetus auratus[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 5 consecutive days
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Result:Achieved 88.4% inhibition of splenic amastigote burden 7 days post-treatment.
Chemical Information
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Molecular Weight 444.57
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Formula C30H28N4
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SMILES
CC(C)(C)NC1=C(N=C2N1C(C3=CC=CC=C3C)=C4C(C5=C(C=CC=C5)N4)=C2)C6=CC=CC=C6
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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-44
- Antileishmanial agent44
- Antileishmanial agent 44
- Parasite
- Sirtuin
- NO Synthase
- TNF Receptor
- Interleukin Related
- Reactive Oxygen Species (ROS)
- oxidative stress
- cytochrome-c
- mitochondrial membrane depolarization
- NAD-dependent deacetylase
- J774A.1 macrophages
- apoptosis-like cell death
- visceral leishmaniasis
- Sir2
- reactive oxygen species
- Leishmania donovani
- Inhibitor
- inhibitor
- inhibit