1. Immunology/Inflammation
  2. NOD-like Receptor (NLR)
  3. NLRP3-IN-16

NLRP3-IN-16 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-16 inhibits IL-1β release with an IC50 of 0.065 μM. NLRP3-IN-16 can be used for the research of inflammation.

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

NLRP3-IN-16 Chemical Structure

NLRP3-IN-16 Chemical Structure

CAS No. : 2906872-59-9

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Description

NLRP3-IN-16 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-16 inhibits IL-1β release with an IC50 of 0.065 μM. NLRP3-IN-16 can be used for the research of inflammation[1].

IC50 & Target[1]

NLRP3 inflammasome

 

In Vitro

NLRP3-IN-16 (Compound 12d) inhibits IL-1β release with an IC50 of 0.065 μM (ELISA assay)[1].
NLRP3-IN-16 (2 μM, 3 h) inhibits the secretion of IL-1β (p17) and caspase-1 (p20) in mice peritoneal macrophages (PMs)[1].
NLRP3-IN-16 inhibits the formation of the NLRP3 inflammasome complex by inhibiting ASC oligomerization[1].
NLRP3-IN-16 shows metabolic stability in both human and mouse liver microsomes (T1/2: 223.5 min; Clint: 6.2act μL/min/mg)[1].

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

Western Blot Analysis[1]

Cell Line: Mice peritoneal macrophages(PMs)
Concentration: 2 μM
Incubation Time: 3 h
Result: Inhibited the secretion of IL-1β (p17) and caspase-1 (p20), without affecting pro-IL-1β and pro-caspase-1.
In Vivo

NLRP3-IN-16 (Compound 12a) (50 mg/kg; i.p.) shows anti-inflammatory effect in septic mouse model[1].

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

Animal Model: LPS-induced inflammatory septic mouse model[1]
Dosage: 50 mg/kg
Administration: i.p.
Result: Decreased the release of IL-1β in mouse serum.
Relieved thickening of the alveolar wall in lung.
Animal Model: Mice[1]
Dosage: 20 or 5 mg/kg
Administration: p.o. or i.v.
Result: Pharmacokinetic profile of NLRP3-IN-15 (compound 12a).
parameter dose (mg/kg) T1/2 (h) Tmax (h) F (%)
PO 20 2.725 0.222 5.0
IV 5 2.772 0.083
Molecular Weight

419.47

Formula

C25H25NO5

CAS No.
SMILES

CC1=C2C=CC3=C(C2=CC=C1)C(C(C4=C3OC5=C4CCN(C5)[C@@H](CCCO)CO)=O)=O

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

Purity & Documentation
References
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NLRP3-IN-16 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.

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NLRP3-IN-16
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HY-149123
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