NLRP3 Inflammasome Inhibitor I

Catalog No.S3680 Batch:S368001

Technical Data

Formula	C₁₆H₁₇ClN₂O₄S
Molecular Weight	368.84	CAS No.	16673-34-0
Solubility (25°C)*	In vitro	DMSO	73 mg/mL (197.91 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

NLRP3 Inflammasome Inhibitor I, an intermediate substrate in the synthesis of glyburide which is free of the cyclohexylurea moiety involved in insulin release, is a novel inhibitor of the NLRP3 inflammasome.

Targets

NLRP3 inflammasome ^[1]

In vitro

NLRP3 Inflammasome Inhibitor I inhibits the formation of the NLRP3 inflammasome in cardiomyocytes without affecting glucose metabolism.^[1]

In vivo

Treatment with 16673-34-0 in a model of acute myocardial infarction because of ischemia and reperfusion significantly inhibites the activity of inflammasome (caspase-1) in the heart by 90% (P < 0.01) and reduces infarct size, measured at pathology (by >40%, P < 0.01) and with troponin I levels (by >70%, P < 0.01).^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines J774A.1 cells, HL-1 cells Concentrations 400μM Incubation Time 30 min Method Cells are cultured in a Claycomb medium and then primed with LPS (25 ng/mL) for 2 h and treated with ATP (5 mM) for 1 hour, to induce NLRP3 inflammasome formation. Cells are then treated with 16673-34-0 (400μM) or glyburide (400μM) during the LPS priming phase and then treated with ATP. The formation of the NLRP3 inflammasome is determined and quantified by ASC aggregation, caspase-1 activity, and cell death.

Cell Assay:^{^[1]}

Cell lines
J774A.1 cells, HL-1 cells
Concentrations
400μM
Incubation Time
30 min
Method
Cells are cultured in a Claycomb medium and then primed with LPS (25 ng/mL) for 2 h and treated with ATP (5 mM) for 1 hour, to induce NLRP3 inflammasome formation. Cells are then treated with 16673-34-0 (400μM) or glyburide (400μM) during the LPS priming phase and then treated with ATP. The formation of the NLRP3 inflammasome is determined and quantified by ASC aggregation, caspase-1 activity, and cell death.

References

[1] Marchetti C, et al. J Cardiovasc Pharmacol. 2014 Apr;63(4):316-322.

Selleck's NLRP3 Inflammasome Inhibitor I has been cited by 8 publications

股関節疾患の病態と治療に関する研究 [ eprints, 2023, 10.14943/doctoral.k15475]	PubMed: none
Inflammasome Activation in the Hip Synovium of Rapidly Destructive Coxopathy Patients and Its Relationship with the Development of Synovitis and Bone Loss [ Am J Pathol, 2022, S0002-9440(22)00076-1]	PubMed: 35292262
Mechanism of miR-126 in hypoxia-reoxygenation-induced cardiomyocyte pyroptosis by regulating HMGB1 and NLRP3 inflammasome [ Immunopharmacol Immunotoxicol, 2022, 1-24]	PubMed: 35297734
Emodin alleviates LPS-induced myocardial injury through inhibition of NLRP3 inflammasome activation [ Phytother Res, 2021, 10.1002/ptr.7191]	PubMed: 34131970
Ginseng Saponin Enriched in Rh1 and Rg2 Ameliorates Nonalcoholic Fatty Liver Disease by Inhibiting Inflammasome Activation [ Nutrients, 2021, 13(3)856]	PubMed: 33807927
Agmatine Alleviates Epileptic Seizures and Hippocampal Neuronal Damage by Inhibiting Gasdermin D-Mediated Pyroptosis [ Front Pharmacol, 2021, 12:627557]	PubMed: 34421582
Emodin alleviates myocardial ischemia/reperfusion injury by inhibiting gasdermin D-mediated pyroptosis in cardiomyocytes. [ Drug Des Devel Ther, 2019, 13:975-990]	PubMed: 30988600
H2S alleviates renal injury and fibrosis in response to unilateral ureteral obstruction by regulating macrophage infiltration via inhibition of NLRP3 signaling. [ Exp Cell Res, 2019, 10.1016/j.yexcr.2019.111779]	PubMed: 31846625

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SHIPPING AND STORAGE
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