NLRP3-IN-8
NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM).
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- No. CAS: 2768650-56-0
- Fòrmula: C23H20N2O6
- Peso molecular:420.41
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Actividad biológica
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NLRP3 |
NLRP3 inflammasome |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
>100 μM
Compound: 27
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 35428012] |
NLRP3-IN-8 (compound 27) exhibits prominent anti-inflammatory activity with an IC50 of 1.23 μM[1].
NLRP3-IN-8 exhibits good metabolic stability through human liver microsomes (t1/2 = 138.63 min)[1].
NLRP3-IN-8 (0-10 μM, 1 h) significantly inhibits pyrolysis rate in a concentration-dependent manner[1].
NLRP3-IN-8 only inhibits the activation of NLRP3 inflammasomes, and could inhibit the activation of inflammasome by a variety of inducer[1].
NLRP3-IN-8 blocks NLRP3-induced ASC oligomerization[1].
NLRP3-IN-8 inhibits NLRP3 inflammasome assembly by blocking the interaction of NLRP3-NEK7 and NLRP3-ASC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDMs cells
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Concentration:0.5, 1, and 2 μM
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Incubation Time:30 min, pretreated with LPS (200 ng/mL) for 3 h
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Result:Dose-dependently blocked IL-1 b secretion and caspase-1 cleavage at concentrations of 0.5-2 μM. Inhibited the maturation of intracellular caspase-1 (p20), and did not affect the expression of other constituent proteins of NLRP3 inflammasome, such as pro-IL-1 β, pro-caspase-1 (p45), NLRP3, ASC and NEK7.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced acute colitis model in C57BL/6 male mice[1].
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Dosage:20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution.
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Administration:Intragastric administration, once a day, 7 days.
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Result:Reduced the weight loss during the onset of colitis in mice, and decreased the disease activity index (DAI) in a dose-dependent manner. Reduced colon shortening, pathological index score, the expression of TNF-a, IL-6 and IL-1 β in the tissues and inhibited the decrease of goblet cells.
Chemical Information
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No. CAS 2768650-56-0
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Peso molecular 420.41
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Fòrmula C23H20N2O6
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SMILES
COC1=CC(OC)=C(C(/C=C/C2=CC=C(C=C2)NC(C3=CC=CO3)=O)=C1)/C=C/[N+]([O-])=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3-IN-8 Related Classifications
HY-146594 Related Classifications
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