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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H17ClN2O4S |
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分子量 | 368.84 | CAS No. | 16673-34-0 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | 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. |
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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] |
細胞アッセイ | 細胞株 | J774A.1 cells, HL-1 cells |
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濃度 | 400μM | |
反応時間 | 30 min | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Acute myocardial infarction (AMI) mouse model ( Adult male CD1 mice ) |
投薬量 | 5mg/kg , 20 mg/kg , 100 mg/kg | |
投与方法 | i.p |
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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