1. Immunology/Inflammation Apoptosis
  2. NOD-like Receptor (NLR) Interleukin Related Caspase
  3. 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.

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NLRP3-IN-91

NLRP3-IN-91 Chemical Structure

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Description

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[1].

IC50 & Target[1]

NLRP3 inflammasome

558.4 nM (Kd)

IL-1β

0.094 μM (IC50)

Caspase-1

 

In Vitro

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.

ELISA Assay[1]

Cell Line: J774A.1 murine macrophages
Concentration: 0.04, 0.12, 0.37, 1.11, 3.33, 10 μM
Incubation Time: 30 min
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.

Western Blot Analysis[1]

Cell Line: J774A.1 murine macrophages
Concentration: 0.2, 1, and
5 μM
Incubation Time: 2.5 h
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.
In Vivo

NLRP3-IN-91 (compound D12) (10 mg/kg; i.p.; single dose; 1 hour pre-LPS) significantly prolongs the survival time of LPS-induced septic mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (8 weeks old, 20-25 g) intraperitoneally injected with LPS (40 mg/kg)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose; 1 hour pre-LPS
Result: Exceeded 40% survival rate at 72 hours post-LPS challenge.
Molecular Weight

576.04

Formula

C27H27ClFN3O6S

SMILES

O=C(N(CC1=CC(Cl)=CC=C1OCCOC)C2=NC3=CC(NS(=O)(CC)=O)=CC=C3O2)CC4=CC=C(F)C=C4

Shipping

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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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.

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Product Name:
NLRP3-IN-91
Cat. No.:
HY-183296
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