Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon acetate induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research[1][2].
Resomelagon acetate（0-1000 μM；8 分钟；HEK293A 细胞）通过 ERK1/2 磷酸化和 Ca2+ 动员促进黑皮质素信号转导[1] 。
Resomelagon acetate（1 nM；30 分钟；腹膜巨噬细胞）具有抗炎活性并抑制 TNF-α 释放和胞吐作用[1]。
Resomelagon acetate（0-10 mg/kg；腹腔注射、静脉注射、口服.；24 小时；雄性 C57BL/6J 野生型 (WT) 和 BALB/c 小鼠）促进体内急性炎症的消退[1 ]。
Resomelagon acetate（25-50 mg/kg；口服；每日一次，持续 8 天；雄性 C57BL/6J 野生型 (WT) 和 BALB/c 小鼠）减少小鼠的关节炎[1]。
[1]. Montero-Melendez T, et, al. Biased agonism as a novel strategy to harness the proresolving properties of melanocortin receptors without eliciting melanogenic effects. J Immunol. 2015 Apr 1;194(7):3381-8.
[2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical.