CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.
CRN04894 selectively blocks the ACTH-MC2R interaction, showing no binding to MC1R, MC3R, MC4R, and MC5R at concentrations >1 uM.
CRN04894 demonstrates remarkable efficacy in a rat model of adrenocorticotrophic hormone (ACTH)-stimulated corticosterone secretion.
Oral administration of CRN04894 suppressed ACTH-stimulated corticosterone secretion in a dose-dependent manner at doses ≥3 mg/kg.
