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).
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- 화학식: C17H14N4O4
- 분자량:338.32
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:LPS (0.1 μg/mL) induced RAW264.7 cells
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Concentration:2.5, 10 μM
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Incubation Time:24 h
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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.
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Cell Line:LPS (0.1 μg/mL) induced RAW264.7 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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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.
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.
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Animal Model:2.6 % DSS induced colitis in male C57BL/6 mice (6-7 weeks)[1]
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Dosage:35 mg/kg
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Administration:Intragastric gavage (i.g.), 9 days
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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.
Chemical Information
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분자량 338.32
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화학식 C17H14N4O4
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SMILES
COC1=CC=C(C2=NC(C(NNC(C3=NC=CC=C3)=O)=O)=CO2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3-IN-76 Related Classifications
HY-170218 Related Classifications
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