NLRP3-IN-87
NLRP3-IN-87 is a selective and orally active NLRP3 inhibitor with a Kd of 0.23 μM. NLRP3-IN-87 binds directly to the NLRP3 NACHT domain, disrupts NLRP3-NEK7 and NLRP3-ASC interactions, inhibits ASC oligomerization, and blocks inflammasome assembly. NLRP3-IN-87 suppresses caspase-1 activation and IL-1β secretion. NLRP3-IN-87 exhibits anti-inflammatory and analgesic activity, reducing joint swelling, inflammation, and pain in an MSU (HY-B2130A)-induced acute gout mouse model. NLRP3-IN-87 can be used for the research of gout.
For research use only. We do not sell to patients.
- CAS No.: 3097745-69-9
- Formula: C21H21BrN2O4S
- Molecular Weight:477.37
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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
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Biological Activity
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NLRP3 0.23 μM (Kd) |
Caspase-1 |
IL-1β |
NLRP3-IN-87 (Compound M48) binds directly to the NACHT domain of purified human NLRP3 protein with a Kd of 0.23 μM[1].
NLRP3-IN-87 (1-20 nM; 30 min pre-incubation prior to nigericin stimulation) potently inhibits NLRP3 inflammasome-mediated IL-1β secretion with an IC50 of 11.9 nM and blocks caspase-1 activation in BMDM cells[1].
NLRP3-IN-87 (50-500 nM) dose-dependently disrupts NLRP3 interactions with NEK7 and ASC in LPS (HY-D1056)/Nigericin (HY-127019)-activated mouse BMDMs[1].
NLRP3-IN-87 (10-100 nM; 30 min pre-incubation prior to nigericin stimulation) dose-dependently inhibits ASC oligomerization and speck formation in LPS/Nigericin-activated mouse BMDMs[1].
NLRP3-IN-87 (0.01-1000 μM; 10-90 min) increases NLRP3 protein thermal stability in a concentration-dependent manner and time-dependent manner in LPS-stimulated mouse BMDM lysates[1].
NLRP3-IN-87 (0-400 μM; 24 h) shows similar low cytotoxicity in human hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDM cells
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Concentration:1, 2, 5, 10 and 20 nM
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Incubation Time:30 min preincubation before LPS
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Result:Reduced IL-1β expression and caspase-1 levels.
NLRP3-IN-87 (100-200 mg/kg; i.g.; daily; 14 days) does not induce significant toxicity in ICR mice, as measured by body weight, organ weight, histopathology, and serum biomarkers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (both male and female, 3- to 5-week-old, gout induced by monosodium urate crystals injection into right footpad)[1]
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Dosage:3 mg/kg
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Administration:p.o.; single dose 0.5 hours before MSU injection
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Result:Significantly reduced the footpad swelling index compared to solvent-treated controls.
Significantly increased the 50% mechanical paw withdrawal threshold compared to solvent-treated controls.
Significantly reduced IL-1β levels in footpad tissues compared to solvent-treated controls.
Chemical Information
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CAS No. 3097745-69-9
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Molecular Weight 477.37
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Formula C21H21BrN2O4S
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SMILES
O=C(NS(=O)(C1=CC(Br)=CC2=C1OCC2)=O)NC3=C4CCCC4=CC5=C3CCC5
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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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