AP1189 acetate

Description

AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages. No melanogenesis was induced by AP1189 in B16-F10 melanocytes. In vivo, oral AP1189 elicited anti-inflammatory actions in peritonitis and, upon administration at the peak of inflammation, accelerated the resolution phase by ～3-fold.

Uses

(E/Z)-Resomelagon acetate is an agonist of melanocortin receptor 1 (MC1R) and MC3R with anti-inflammatory activities. (E/Z)-Resomelagon can be utilized in inflammation research[1].

IC 50

MC1R; MC3R

References

[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. DOI:10.4049/jimmunol.1402645