1. GPCR/G Protein Neuronal Signaling
  2. Melanocortin Receptor
  3. BMS-470539

BMS-470539 是一种合成的 MC-1R 激动剂,具有强大的抗炎特性。BMS-470539 选择性地激活人类和鼠类 MC-1R,EC50 值分别为 16.8 nM 和 11.6 nM。体外研究表明,BMS-470539 能够剂量依赖性地抑制表达 MC-1R 的人类黑色素瘤细胞中 TNF-alpha 诱导的 NF-kB 激活。在体内,给 BALB/c 小鼠皮下注射 BMS-470539 可有效抑制 LPS 诱导的 TNF-alpha 产生,ED50 约为 10 μmol/kg,药效学半衰期约为 8 小时。它还显著减少了肺部炎症模型中的白细胞浸润,减轻了迟发型超敏反应模型中的爪肿胀,突出了其通过 MC-1R 调节作为抗炎剂的功效。

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BMS-470539 Chemical Structure

BMS-470539 Chemical Structure

CAS No. : 457893-92-4

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生物活性

BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation[1].

分子量

559.70

Formula

C32H41N5O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BMS-470539
目录号:
HY-15616
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