1. Immunology/Inflammation NF-κB
  2. NOD-like Receptor (NLR) Interleukin Related NF-κB NO Synthase
  3. NLRP3-IN-76

NLRP3-IN-76 is an orally active NLRP3 inhibitor. NLRP3-IN-76 inhibits the production of NO, and the mRNA levels of proinflammatory cytokines (iNOS, IL-6, IL-1β and TNFα). NLRP3-IN-76 shows anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and NF-κB signaling pathway. NLRP3-IN-76 ameliorates DSS (HY-116282C)-induced colitis and can be used for research of inflammatory bowel diseases (IBD).

For research use only. We do not sell to patients.

NLRP3-IN-76 Chemical Structure

NLRP3-IN-76 Chemical Structure

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Description

NLRP3-IN-76 is an orally active NLRP3 inhibitor. NLRP3-IN-76 inhibits the production of NO, and the mRNA levels of proinflammatory cytokines (iNOS, IL-6, IL-1β and TNFα). NLRP3-IN-76 shows anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and NF-κB signaling pathway. NLRP3-IN-76 ameliorates DSS (HY-116282C)-induced colitis and can be used for research of inflammatory bowel diseases (IBD)[1].

In Vitro

NLRP3-IN-76 (Compound ST12) (10 μM, 24 h) inhibits nitric oxide (NO) production (52.67%) in LPS induced RAW264.7 cells[1].
NLRP3-IN-76 (10 μM, 24 h) inhibits mRNA levels of proinflammatory cytokines in LPS-stimulated RAW264.7 cells, such as inducible NO synthase (iNOS), IL-6, IL-1β and TNF-α[1].
NLRP3-IN-76 (2.5-10 μM, 24 h) inhibits NLRP3 inflammasome activation and NF-κB signaling pathway in LPS-stimulated RAW264.7 cells [1].

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

RT-PCR[1]

Cell Line: LPS (0.1 μg/mL) induced RAW264.7 cells
Concentration: 2.5, 10 μM
Incubation Time: 24 h
Result: Significantly inhibited the mRNA levels of inflammatory factors (iNOS, IL-6, IL-1β and TNF-α) at 10 μM.
Inhibited the mRNA levels of IL-6, IL-1β at 2.5 μM.

Western Blot Analysis[1]

Cell Line: LPS (0.1 μg/mL) induced RAW264.7 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Dose-dependently downregulated the expression of p-IκBα and p-p65 without affecting IκBα and p65.
Downregulated the expression of NLRP3.
Inhibited the expression of caspase-1, IL-18 and GSDMD.
In Vivo

NLRP3-IN-76 (Compound ST12) (35 mg/kg, i.g., 9 days) protects mice from DSS-induced colitis by inhibiting the in vivo activation of NLRP3 inflammasome[1].
NLRP3-IN-76 (100-400 mg/kg, p.o.) is well-tolerated in the C57 mice (LD50: 300 mg/kg)[1].

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

Animal Model: 2.6 % DSS induced colitis in male C57BL/6 mice (6-7 weeks)[1]
Dosage: 35 mg/kg
Administration: Intragastric gavage (i.g.), 9 days
Result: Increased the colon lengths (6.09 cm) compared to the DSS-induced colitis model group (4.39 cm).
Alleviated the DSS-induced reduction in crypt numbers and depletion of goblet cells.
Reduced DSS-induced CD86-positive cells.
Reduced the p-IκBα and p-p65 levels in colonic tissues.
No significant organ toxicity was observed.
Molecular Weight

338.32

Formula

C17H14N4O4

SMILES

COC1=CC=C(C2=NC(C(NNC(C3=NC=CC=C3)=O)=O)=CO2)C=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
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  • 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-76
Cat. No.:
HY-170218
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