NLRP3-IN-75
NLRP3-IN-75 is an orally active NLRP3 inhibitor. NLRP3-IN-75 suppresses IL-1β secretion (IC50 = 23 nM). NLRP3-IN-75 selectively inhibits NLRP3 activation by disrupting inflammasome assembly without affecting NLRC4 or AIM2 inflammasomes. NLRP3-IN-75 exhibits superior efficacy in acute peritonitis, diabetic kidney disease and IBD models.
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- Formule: C20H30N4O3S
- Masse moléculaire:406.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
IC50 & Target
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IL-1β 23 nM (IC50) |
In Vitro
NLRP3-IN-75 (Compound 15) (0.03-100 μM, 30 min) significantly inhibits IL-1β release in LPS- and ATP-stimulated BMDM cells (IC50 = 0.106 μM) and THP-1 cells (IC50 = 23 nM)[1].
NLRP3-IN-75 (10 μM, 4 h) shows selectivity for NLRP3 inflammasome by maintaining IL-1β secretion in the NLRC4 or AIM2 inflammasome pathways in flagellin-transfected BMDM cells[1].
NLRP3-IN-75 (10 μM, 4 h) does not affect the initiation phase of NLRP3 inflammation activation as TNF-α and IL-6 production maintains[1].
NLRP3-IN-75 (10 μM, 4 h) obstructs the interaction between NLRP3 and ASC induced by LPS and ATP in BMDM cells by impeding NLRP3 inflammasome assembly[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
NLRP3-IN-75 (20 mg/kg, p.o., 6 weeks) mitigates HFD- and STZ-induced DKD in mice by targeting the NLRP3 inflammasome [1].
NLRP3-IN-75 (0.2-5 mg/kg, p.o., 10 days) ameliorates the DSS (HY-116282C)-induced inflammatory bowel disease in mice models[1].
NLRP3-IN-75 (20 mg/kg, p.o., a single dose) shows low potential for cardiovascular or pulmonary toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS (HY-D1056) (15 mg/kg, i.p.)- and ATP (1 mM/kg, i.p.)-induced acute peritonitis mice (6-8 weeks old, male C57BL/6J)[1]
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Dosage:1 mg/kg, 20 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Achieved 100% survival rate in LPS-induced followed by ATP-induced acute peritonitis mice models.
Suppressed serum IL-1β level in peritonitis mice models 12 h post-ATP administration, and presented better effect with increasing dose.
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Animal Model:Male C57BL/6J HFD (4 weeks)- and STZ (HY-13753) (50 mg/kg, i.p., 5 days)-induced diabetic kidney disease (DKD) mice (n = 5-6, 20-22 g)[1]
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Dosage:20 mg/kg, 6 weeks
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Administration:Oral gavage (p.o.), 6 weeks; administered after STZ and HFD feeding
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Result:Significantly reduced the elevated urine albumin-to-creatinine ratio (UACR) caused by the HFD- and STZ-induced DKD mice models.
Ameliorated the thickening of the glomerular and tubular basement membranes in DKD models.
Decreased inflammatory cytokine IL-1β but no effect on TNF-α level[1].
Reduced macrophage infiltration.
Disrupted the NLRP3-ASC interaction.
Reduced LDL-C levels without affecting HDL-C levels.
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Animal Model:2% (w/v) DSS (HY-116282C) (7 days) in distilled water-induced colitis mice (Male C57BL/6J, n = 5-10, 20-22 g)[1]
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Dosage:0.2 or 5 mg/kg
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Administration:Oral gavage (p.o.) , 9 days (day 1-day 10)
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Result:Attenuated weight loss in DSS-induced acute colitis mice models.
Reduced fecal bleeding and decreased disease activity index (DAI) scores.
Ameliorated pathological features such as disruption of mucosal barrier, crypt necrosis, substantial depletion of the mucosal barrier, crypt necrosis, substantial depletion of goblet cells, and pronounced infiltration of inflammatory cells.
Inhibited colonic IL-1β without affecting TNF-α level.
Chemical Information
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Masse moléculaire 406.54
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Formule C20H30N4O3S
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SMILES
O=C(NC1=C2CCCC2=CC3=C1CCC3)NS(N(C4CCN(CC4)C)C)(=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3-IN-75 Related Classifications
HY-170233 Related Classifications
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