产品
编 号:F747258
分子式:C14H14N6O2
分子量:298.3
产品类型
结构图
CAS No: 1809420-71-0
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产品详情
生物活性:
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.
体内研究:
Resomelagon(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(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。Animal Model:Male C57BL/6J wild-type (WT) and BALB/c mice
Dosage:0, 0.1, 1 and 10 mg/kg
Administration:Oral administration, intraperitoneal injection and intravenous injection; for 24 hours
Result:Inhibited neutrophil and monocyte infiltration in a dose-dependent manner.
Animal Model:Male C57BL/6J wild-type (WT) and BALB/c mice
Dosage:25 and 50 mg/kg
Administration:Oral administration; daily; for 8 days
Result:Reduced all signs of arthritis measured, including clinical score (-42%), paw swelling (-87%), proportion of animals with all four paws affected (-50%), and the severity of the inflammation (-70%).
体外研究:
Resomelagon(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 。Resomelagon(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。