OXGR1 agonist A-1 is a potent and selective OXGR1 (Oxoglutarate Receptor 1, GPR99) agonist, activates Gq signaling of OXGR1 with EC50 of 626.5 nM.
A-1 activates OXGR1 with a potency approximately 60 times stronger compared with α-KG.
A-1 shows no detectable activity for GPR91.
OXGR1-F113L mutant reduced the potency of A-1 by more than 10,000-fold.
A-1 promoted phosphorylation of MYL9 and MLCK expression in VSMCs comparable to α-KG.
A-1 (80 uM) obviously improved rosacea-related phenotypes when applied topically to the back skins of mice.
A-1 mitigates erythema and inflammation with efficacy comparable to first-line therapy while offering enhanced safety in rosacea-like models.
