2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Caspase Interleukin Related
  4. 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.

NLRP3-IN-87

NLRP3-IN-87 Chemical Structure

CAS No. : 3097745-69-9

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NLRP3-IN-87 Related Antibodies

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Description

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[1].

IC50 & Target[1]

NLRP3

0.23 μM (Kd)

Caspase-1

 

IL-1β

 

In Vitro

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.

NLRP3-IN-87 Related Antibodies

Western Blot Analysis[1]

Cell Line: BMDM cells
Concentration: 1, 2, 5, 10 and 20 nM
Incubation Time: 30 min preincubation before LPS
Result: Reduced IL-1β expression and caspase-1 levels.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-∞ Vd CL F
Rat[1] 3 mg/kg i.v. 3.9 h 0.03 h 37840.5 ng/mL 41089.3 ng·h/mL 413.5 mL/kg 75.4 mL/h/kg /
Rat[1] 20 mg/kg p.o. 6.3 h 4.00 h 25515.7 ng/mL 245671.3 ng·h/mL 649.9 mL/kg 84.4 mL/h/kg 89.7 %
In Vivo

NLRP3-IN-87 (Compound M48) (3 mg/kg; i.g.; single dose 0.5 hours before MSU injection) significantly reduces MSU (HY-B2130A)-induced foot swelling, mechanical pain, and IL-1β levels in an ICR mouse gout model[1].
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.

Animal Model: ICR (both male and female, 3- to 5-week-old, gout induced by monosodium urate crystals injection into right footpad)[1]
Dosage: 3 mg/kg
Administration: p.o.; single dose 0.5 hours before MSU injection
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.
Molecular Weight

477.37

Formula

C21H21BrN2O4S
CAS No.
SMILES

O=C(NS(=O)(C1=CC(Br)=CC2=C1OCC2)=O)NC3=C4CCCC4=CC5=C3CCC5
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-87 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-873097745-69-9NOD-like Receptor (NLR)CaspaseInterleukin RelatedILhepatocytesliver microsomesSprague-Dawley Ratscaspase-1NEK7NLRP3 NACHT domainMSUgoutASCIL-1βBMDMsInhibitorinhibitorinhibit

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