ZM734
ZM734 is an orally active and selective NLRP3 inflammasome inhibitor. ZM734 inhibits the secretion of IL-1β. ZM734 alleviates pulmonary inflammation in a mouse model of acute lung injury. ZM734 can be used for the research of inflammatory diseases such as acute lung injury.
For research use only. We do not sell to patients.
- CAS No.: 3068219-50-8
- Formula: C19H20FN3O3S
- Molecular Weight:389.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IL-1β |
ZM734 (0.1-2000 nM; 1 h) potently and selectively inhibits NLRP3 inflammasome activation in mouse bone marrow-derived macrophages (BMDMs), with an IC50 value of 400 nM for IL-1β and 721 nM for IL-18, while exerting no effect on TNF-α, IL-6, AIM2 and NLRC4 pathways[1].
The CC50 of ZM734 in BMDMs is 92.0 μM[1].
ZM734 (0.1-1 μM) inhibits the production of IL-1β in human THP-1 cells[1].
ZM734 (1 μM) inhibits the expression of pro-IL-1β without altering the levels of NLRP3 or pro-caspase-1 in BMDMs stimulated with LPS (HY-D1056) + ATP (HY-B2176), and it acts on the activation stage of the NLRP3 inflammasome[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDMs
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Concentration:0.1-10 μM; 64.5-2000 nM
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Incubation Time:1 h (pre-incubation prior to LPS stimulation)
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Result:Inhibited LPS+ATP-induced IL-1β secretion by 59.1% at 0.1 μM.
Inhibited LPS+ATP-induced IL-1β secretion by 69.5% at 1 μM.
Exhibited dose-dependent inhibition of LPS+ATP-induced IL-1β and IL-18 secretion, with IC50 values of 400 nM and 721 nM, respectively.
Did not significantly inhibit LPS-induced TNF-α or IL-6 secretion at 1 μM and 10 μM.
Significantly reduced IL-1β secretion induced by multiple NLRP3 activators (LPS+ATP, LPS+Nigericin, LPS+MSU).
Showed no significant inhibitory effect on AIM2 or NLRC4 inflammasome-mediated IL-1β secretion.
ZM734 (30-60 mg/kg; p.o.; single dose) exhibits reduced hepatotoxicity in healthy C57BL/6 mice, causing smaller elevations in serum ALT and AST levels than MCC950 at equivalent or higher oral doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (n=6 per group)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly alleviated LPS-induced lung pathological injuries, including reductions in inflammatory cell infiltration, intravascular congestion, alveolar wall thickening, and pulmonary interstitial hemorrhage.
Significantly suppressed LPS-induced increases in IL-1β levels in mouse bronchoalveolar lavage fluid, with no significant effect on TNF-α or IL-6 levels.
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Animal Model:C57BL/6 mice (8 weeks old; equal numbers of males and females; n=6 per group)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; single dose
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Result:Induced smaller increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared to MCC950 at the same 30 mg/kg dose.
Caused ALT and AST levels that remained lower than those induced by MCC950 at 30 mg/kg when administered at 60 mg/kg.
Chemical Information
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CAS No. 3068219-50-8
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Molecular Weight 389.44
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Formula C19H20FN3O3S
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SMILES
FC1=CC(S(N/C(NC2=C3C(CCC3)=CC4=C2CCC4)=N\O)(=O)=O)=CC=C1
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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)
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