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CT-859 is a unimolecular, fully cAMP-biased dual glucagon-like peptide-1 receptor (GLP-1R) and gastric inhibitory polypeptide receptor (GIPR) agonist. Developed initially by Carmot Therapeutics (subsequently acquired by Roche), CT-859 is engineered to selectively stimulate cAMP signaling without recruiting beta-arrestin-1 or beta-arrestin-2, thereby preventing receptor internalization and desensitization. It serves as a mouse analogue of CT-868 and has demonstrated prolonged food intake suppression, glycemic control, and weight loss in preclinical rodent models of obesity, type 2 diabetes, and metabolic dysfunction-associated steatohepatitis (MASH).
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