2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. 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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NLRP3-IN-8 Chemical Structure

NLRP3-IN-8 Chemical Structure

CAS No. : 2768650-56-0

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NLRP3-IN-8 Related Antibodies

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Description

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)[1].

IC50 & Target

NLRP3

 

NLRP3 inflammasome

 

Cellular Effect
Cell Line Type Value Description References
L02 IC50
> 100 μM
Compound: 27
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
[PMID: 35428012]
In Vitro

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.

NLRP3-IN-8 Related Antibodies

Western Blot Analysis[1]

Cell Line: BMDMs cells
Concentration: 0.5, 1, and 2 μM
Incubation Time: 30 min, pretreated with LPS (200 ng/mL) for 3 h
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.
In Vivo

NLRP3-IN-8 (compound 27) (DSS-induced C57BL/6 male mice; 0-20 mg/kg; intragastric; once a day, 7 days) effectively alleviates the severity of DSS-induced colitis in mouse[1].

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

Animal Model: DSS-induced acute colitis model in C57BL/6 male mice[1].
Dosage: 20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution.
Administration: Intragastric administration, once a day, 7 days.
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.
Molecular Weight

420.41

Formula

C23H20N2O6
CAS No.
SMILES

COC1=CC(OC)=C(C(/C=C/C2=CC=C(C=C2)NC(C3=CC=CO3)=O)=C1)/C=C/[N+]([O-])=O
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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NLRP3-IN-8 Related Classifications

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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.

Keywords:

NLRP3-IN-82768650-56-0NOD-like Receptor (NLR)BMDMsDSS-induced colitisNLRP3 inflammasomeInhibitorinhibitorinhibit

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