NLRP3-IN-91
NLRP3-IN-91 is a potent NLRP3 inflammasome inhibitor with a Kd of 558.4 nM. NLRP3-IN-91 directly targets the NLRP3 NACHT domain, blocks inflammasome assembly and activation, and exerts anti-inflammatory effects. NLRP3-IN-91 increases survival time in a murine model of LPS (HY-D1056)-induced sepsis. NLRP3-IN-91 can be used for the research of sepsis.
For research use only. We do not sell to patients.
- Formula: C27H27ClFN3O6S
- Molecular Weight:576.04
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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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Biological Activity
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NLRP3 inflammasome 558.4 nM (Kd) |
IL-1β 0.094 μM (IC50) |
Caspase-1 |
NLRP3-IN-91 (compound D12) (0.04-10 μM; 30 min) potently inhibits NLRP3 inflammasome-mediated IL-1β secretion in J774A.1 murine macrophages with an IC50 of 0.094 μM[1].
NLRP3-IN-91 (24 h) shows low cytotoxicity in vitro, with CC50 values >30 μM in J774A.1 murine macrophages and >100 μM in AML-12 mouse normal hepatocytes[1].
NLRP3-IN-91 (0.2-5 μM; 2.5 h) dose-dependently inhibits NLRP3 inflammasome assembly and activation in J774A.1 murine macrophages by reducing cleaved caspase-1 (p20) and mature IL-1β production[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J774A.1 murine macrophages
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Concentration:0.04, 0.12, 0.37, 1.11, 3.33, 10 μM
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Incubation Time:30 min
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Result:Inhibited IL-1β secretion by 80.2% at 1 μM.
Inhibited IL-1β secretion by 96.6% at 10 μM.
Exhibited an IC50 of 0.094 μM for NLRP3 inflammasome-mediated IL-1β release.
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Cell Line:J774A.1 murine macrophages
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Concentration:0.2, 1, and
5 μM -
Incubation Time:2.5 h
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Result:Suppressed the production of cleaved caspase-1 (p20 subunit) and mature IL-1β in a dose-dependent manner.
Did not affect levels of pro-caspase-1, pro-IL-1β, NLRP3, or GAPDH.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8 weeks old, 20-25 g) intraperitoneally injected with LPS (40 mg/kg)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose; 1 hour pre-LPS
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Result:Exceeded 40% survival rate at 72 hours post-LPS challenge.
Chemical Information
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Molecular Weight 576.04
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Formula C27H27ClFN3O6S
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SMILES
O=C(N(CC1=CC(Cl)=CC=C1OCCOC)C2=NC3=CC(NS(=O)(CC)=O)=CC=C3O2)CC4=CC=C(F)C=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)
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