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

NLRP3-IN-8 

Cat. No.: HY-146594
Handling Instructions

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).

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

NLRP3-IN-8 Chemical Structure

NLRP3-IN-8 Chemical Structure

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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 inflammasome

 

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].

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

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].

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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NLRP3-IN-8
Cat. No.:
HY-146594
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