2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NLRP3-IN-14

NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation.

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NLRP3-IN-14 Chemical Structure

NLRP3-IN-14 Chemical Structure

CAS No. : 2767369-80-0

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NLRP3-IN-14 Related Antibodies

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Description

NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation[1].

IC50 & Target[1]

NLRP3 inflammasome

5.87 μM (Kd)

In Vitro

NLRP3-IN-14 (Compound 5j) inhibits IL-1β release with an IC50 of 0.131 μM (ELISA assay)[1].
NLRP3-IN-14 (2 μM, 3 h) inhibits the secretion of IL-1β (p17) and caspase-1 (p20) in mice peritoneal macrophages (PMs)[1].
NLRP3-IN-14 inhibits the formation of the NLRP3 inflammasome complex by inhibiting ASC oligomerization[1].
NLRP3-IN-14 (10 μM, 5 h) inhibits the degradation of protein NLRP3 with increasing temperature[1].
NLRP3-IN-14 shows metabolic stability in both human and mouse liver microsomes (T1/2: 866.3 min; Clint: 1.6 μL/min/mg)[1].

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

NLRP3-IN-14 Related Antibodies

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-14 (Compound 5j) (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-14 (compound 5j).
parameter dose (mg/kg) T1/2 (h) Tmax (h) F (%)
PO 20 9.225 0.389 3.0
IV 5 5.028 0.083
Molecular Weight

444.52

Formula

C27H28N2O4
CAS No.
SMILES

CC1=C2C=CC3=C(C2=CC=C1)C(C(C4=C3OC5=C4CCN(C5)CCCN6CCOCC6)=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-14 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-142767369-80-0NOD-like Receptor (NLR)InflammasomeIL-1βinflammationperitoneal macrophageseptic mouseLPSInhibitorinhibitorinhibit

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