2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NLRP3-IN-12

NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease.

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

NLRP3-IN-12 Chemical Structure

NLRP3-IN-12 Chemical Structure

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NLRP3-IN-12 Related Antibodies

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Description

NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease[1].

IC50 & Target

NLRP3 inflammasome[1]
In Vitro

NLRP3-IN-12 (compound 6E) (0.5-2 μM; pretreated for 1 h) inhibits LPS/ATP-stimulated expression of cleaved caspase-1 and IL-1β in THP-M cells[1].
NLRP3-IN-12 (2 μM) inhibits GSDMD-mediated pyroptosis in THP-M cells[1].
NLRP3-IN-12 (1 μM) exhibits the half-life (T1/2) are 53.4 min and 31.8 min in human and rat liver microsomes, respectively[1].

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

NLRP3-IN-12 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-M cells
Concentration: 0.5, 1, 2 μM
Incubation Time: Pretreated for 1 h, then stimulated with LPS (1 μg/mL) for 4.5 h, and ATP (5 mM) for 0.5 h.
Result: Reduced the secretion of IL-1β and caspase-1.
Had no effect on the levels of NLRP3, pro-IL-1β, ASC, pro-caspase 1, p65, p-p65, IκBα, and p-IκBα.
In Vivo

NLRP3-IN-12 (compound 6E) (5-10 mg/kg; i.p. daily for 10 d) attenuates DSS-induced colitis severity in mice[1].
NLRP3-IN-12 (20 mg/kg; i.v.) exhibits the half-life (T1/2) is 6.64 h, elimination rate constant (Kel) is 0.107 h, clearance rate (CL) is 105 mL/kg/min and steady-state apparent volume of distribution (Vdss) is 23.1 L/kg in rats[1].

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

Animal Model: C57BL/6 mice were induced acute colitis by drinking 3% DSS (dextran sulfate sodium)[1]
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection daily for 10 days in aqueous solution containing DMSO/0.5% CMC-Na/normal saline
Result: Attenuated DSS-induced weight loss, loose stools, bloody stools, shortened colons, increased disease activity index score, and lower survival rate.
Molecular Weight

518.00

Formula

C27H32ClNO7
SMILES

O[C@@H]1[C@]2(CO3)[C@@]([C@H](O)[C@]3(O)[C@]45[C@@]2([H])CC[C@](C(C5=O)=C)([H])[C@@]4([H])OC(NC6=CC=CC(Cl)=C6)=O)([H])C(C)(C)CC1
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-12 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-12NOD-like Receptor (NLR)inflammasomeIL-1βinflammatory bowel diseaseInhibitorinhibitorinhibit

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