Resomelagon (C09-1167-585)

Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC 1 and MC 3 . Resomelagon induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation researchIn VitroResomelagon (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HEK293A cells Concentration: 0-1000 μM Incubation Time: 8 minutes Result: Increased the expression of ERK1/2 phosphorylation in a dose-dependent manner.In VivoResomelagon (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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%).Form:SolidIC50& Target:MC1R MC3R. Molecular Formula: C14H14N6O2 Molecular Weight: 298.3 PubChem CID: 23728926 Isomeric SMILES: C1=CC=C(C(=C1)N2C=CC=C2/C=C/C=N/N=C(N)N)[N+](=O)[O-]