2. Immunology/Inflammation
  3. NOD-like Receptor (NLR) Interleukin Related
  4. 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.

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ZM734

ZM734 Chemical Structure

CAS No. : 3068219-50-8

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ZM734 Related Antibodies

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1].

IC50 & Target[1]

IL-1β

 

In Vitro

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.

ZM734 Related Antibodies

ELISA Assay[1]

Cell Line: BMDMs
Concentration: 0.1-10 μM; 64.5-2000 nM
Incubation Time: 1 h (pre-incubation prior to LPS stimulation)
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.
In Vivo

ZM734 (10 mg/kg; i.p.; single dose) exerts a protective effect against LPS-induced acute lung injury in C57BL/6 mice, significantly reducing pulmonary inflammation and IL-1β levels while sparing TNF-α and IL-6 production[1].
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.

Animal Model: C57BL/6 mice (n=6 per group)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: C57BL/6 mice (8 weeks old; equal numbers of males and females; n=6 per group)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

389.44

Formula

C19H20FN3O3S
CAS No.
SMILES

FC1=CC(S(N/C(NC2=C3C(CCC3)=CC4=C2CCC4)=N\O)(=O)=O)=CC=C1
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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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ZM734 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:

ZM7343068219-50-8ZM 734ZM-734NOD-like Receptor (NLR)Interleukin RelatedILmouse bone marrow-derived macrophagesAIM2 inflammasomeshuman THP-1 cellsmouse serum ASTNLRP3 inflammasomehuman hepatic stellate cellsIL-1βNLRC4 inflammasomesmouse serum ALTacute lung injuryInhibitorinhibitorinhibit

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