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.
For research use only. We do not sell to patients.
- CAS No.: 2767369-80-0
- Formula: C27H28N2O4
- Molecular Weight:444.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NLRP3 inflammasome 5.87 μM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| Peritoneal macrophage | IC50 |
0.131 μM
Compound: 5j
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Antiinflammatory activity against LPS-stimulated mouse peritoneal macrophage assessed as inhibition of IL-1beta secretion treated for 3 hrs followed by ATP addition measured after 30 mins by ELISA method
Antiinflammatory activity against LPS-stimulated mouse peritoneal macrophage assessed as inhibition of IL-1beta secretion treated for 3 hrs followed by ATP addition measured after 30 mins by ELISA method
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[PMID: 36786612] |
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.
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Cell Line:Mice peritoneal macrophages(PMs)
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Concentration:2 μM
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Incubation Time:3 h
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Result:Inhibited the secretion of IL-1β (p17) and caspase-1 (p20), without affecting pro-IL-1β and pro-caspase-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced inflammatory septic mouse model[1]
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Dosage:50 mg/kg
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Administration:i.p.
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Result:Decreased the release of IL-1β in mouse serum.
Relieved thickening of the alveolar wall in lung.
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Animal Model:Mice[1]
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Dosage:20 or 5 mg/kg
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Administration:p.o. or i.v.
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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
Chemical Information
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CAS No. 2767369-80-0
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Molecular Weight 444.52
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Formula C27H28N2O4
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SMILES
CC1=C2C=CC3=C(C2=CC=C1)C(C(C4=C3OC5=C4CCN(C5)CCCN6CCOCC6)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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