Bioactivity | 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]. |
Target | Targrt: MC1 and MC3 |
Invitro | Resomelagon (AP1189) (0-1000 μM; 8 min; HEK293A cells) promotes melanocortin signal transduction through ERK1/2 phosphorylation and Ca2+ mobilization[1].Resomelagon (AP1189) (1 nM; 30 min; peritoneal macrophages) has anti-inflammatory activity and inhibits TNF-α release and efferocytosis[1]. Western Blot Analysis[1] Cell Line: |
In Vivo | Resomelagon (AP1189) (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 (AP1189) (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]. Animal Model: |
Name | Resomelagon |
CAS | 1809420-71-0 |
Formula | C14H14N6O2 |
Molar Mass | 298.30 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. [2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical |