Paltusotine CAS# 2172870-89-0 3-(4-(4-氨基哌啶-1-基)-3-(3,5-二氟苯基)喹啉-6-基)-2-羟基苯腈

Paltusotine (CRN00808) is a potent, selective, orally bioavailable non-peptide somatostatin receptor 2 (SST2) agonist with an EC₅₀ of ~0.25 nM and >4,000-fold selectivity over other somatostatin subtypes. It showed good oral exposure in rats and dogs without significant CYP or hERG inhibition. In preclinical pharmacodynamic studies, oral paltusotine dose-dependently suppressed growth hormone (GH) secretion after GHRH challenge in male and female rats and, with repeated dosing, reduced circulating IGF-1 in both rats and dogs. These data validated potent SST2 engagement and endocrine modulation supportive of its development for acromegaly and related disorders.