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BMS-470539 dihydrochloride

產品活性：BMS-470539 dihydrochloride 是一種高效的選擇性黑皮質素 1 受體 (MC-1 R) 激動劑，IC₅₀ 為 120 nM，EC₅₀ 為 28 nM。BMS-470539 dihydrochloride 不激活 MC-3R，并且對 MC-4R 和 MC-5R 的激活活性非常弱。BMS-470539 dihydrochloride 具有強效的抗炎特性。

研究領域：GPCR/G Protein  |  Neuronal Signaling

作用靶點：Melanocortin Receptor

In Vitro: An HBL melanoma cell line is established that stably expresses a NF-κB luciferase reporter. In these cells, 0.5 ng/mL TNF-α induces a dose-dependent increase in NF-κB luciferase activity. Treatment of HBL-NF-κB cells with BMS-470539 elicits a dose-dependent, statistically significant reduction in TNF-α-stimulated NF-κB luciferase activity. BMS-470539 has no effect on luciferase reporter activity in the absence of TNF-α stimulation. In nontransfected HBL cells, treatment with BMS-470539 results in a dose-dependent inhibition of NF-B nuclear translocation.

In Vivo: BMS-470539 (2.05-18.47 mg/kg; intravenous injection; for 125 minutes; WT and MC1 receptor recessive e/e mice) treatment inhibits cell adhesion and emigration with no effect on cell rolling. And also inhibits the tissue expression of both CXCL1 and CCL2.

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