hydrocotarnine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

氢化可塔宁是 Cbl 的抑制剂。

hydrocotarnine?is an inhibitor of Cbl.(In Vivo):In vivo, inhibition of Cbl with an analgesic drug, hydrocotarnine, increases inflammasome-mediated IL-18 secretion in the colon, and protects mice from dextran sulphate sodium-induced colitis. Together, our novel findings provide new insights into the role of the SFK-Cbl axis in suppressing NLRP3 inflammasome activation and identify a novel clinical utility of hydrocortanine for disease treatment.

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. Western Blot Analysis Cell 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.

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. 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.

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Others

Other Targets

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550-10-7

221.25

C12H15NO3

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (451.98 mM)

CN(CC1)Cc2c1cc1OCOc1c2OC

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(-20℃)

With Ice Pack

≥ 2 years