Resomelagon

• CAT Number: I043390
• CAS Number: 1809420-71-0
• Molecular Formula: C14H14N6O2
• Molecular Weight: 298.30
• Purity: ≥95%
• Synonyms: 2-[(E)-[(E)-3-[1-(2-nitrophenyl)pyrrol-2-yl]prop-2-enylidene]amino]guanidine
• InChI: InChI=1S/C14H14N6O2/c15-14(16)18-17-9-3-5-11-6-4-10-19(11)12-7-1-2-8-13(12)20(21)22/h1-10H,(H4,15,16,18)/b5-3+,17-9+
• InChIKey: ZSDGHWLLLGYAJV-AHEHSYJASA-N
• SMILES: C1=CC=C(C(=C1)N2C=CC=C2C=CC=NN=C(N)N)[N+](=O)[O-]

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[1][2].
Resomelagon (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca2+ mobilization[1].
Resomelagon (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis[1].
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[1].
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[1].

Reference

[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.
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[2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical