Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic
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Product Description
Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect in cancer research
In Vitro
Hydrocotarnine is an analgesic agent (CRIN-2), with the patent ID of WO2011160016A2. Hydrocotarnine (10 μM; 1 h) elevates the secretion of IL-1β and IL-18, and (0.1-10 μM; 1 h) increases the global level of tyrosine-phosphorylated proteins in THP-1 cells. Hydrocotarnine (50 μM; 0-100 min) increases the glycolytic capacity and glycolytic reserve capacity in THP-1-derived macrophages. Hydrocotarnine (50 μM; 16 h) inhibits Cbl and increases the total GLUT1 protein in THP-1-derived macrophages. Hydrocotarnine is known to enhance the analgesic effect of opioids, and alleviates cancer pain. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: THP-1 cells Concentration: 0.1, 1, 10 μM Incubation Time: 1 hour Result: Induced p-Pyk2 loss and increased the level of tyrosine-phosphorylated proteins in a dose-dependent manner.
In Vivo
Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) shows inhibitory effect on Cbl and results in increasing IL-18 levels, indicating that NLRP3 inflammasome activation is enhanced in mice . Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) protects mice from DSS-induced colitis, with low scores of pathological evaluation of inflammation, epithelial defects, and crypt atrophy . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: DSS-induced colitis model in C57BL/6 mice (6-9 weeks old) Dosage: 10 mg/kg Administration: Intraperitoneal injection; once daily; 9 days while 2.5% DSS treatment began on day 1 and ended on day 7 Result: Significantly attenuated the weight loss of DSS-induced colitis mice compared to PBS-treated control mice, indicating that decreasing negative regulation of the NLRP3 inflammasome activation could attenuate colitis in an animal model.
This compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
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1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
