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CAS No. : 1809420-71-0
MCE 国际站:Resomelagon
产品活性:Resomelagon (AP1189) 是一种口服有效的黑素皮质素受体 (MR) 激动剂,包括 MC1 and 和MC3。Resomelagon 诱导 ERK1/2 磷酸化和 Ca2+ 流动。Resomelagon 具有抗炎活性。Resomelagon 可用于肥胖和慢性炎症研究。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Melanocortin Receptor
In Vitro: Resomelagon (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca2+ mobilization.
Resomelagon (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis.
In Vivo: Resomelagon (0-10 mg/kg; i.p., i.v. and p.o.; for 24 h; male C57BL/6J wild-type (WT) and BALB/c mice) promotes resolution of acute inflammation in vivo.
Resomelagon (25-50 mg/kg; p.o.; daily, for 8 d; male C57BL/6J wild-type (WT) and BALB/c mice) reduces arthritis in mice.
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