CGP42112

CGP42112 is a synthetic small molecule peptidomimetic that acts as a selective, high affinity full agonist of the angiotensin II type 2 receptor (AT2R). It was first developed by Ciba-Geigy in 1989. The compound's pharmacological activity includes mimicking angiotensin II-mediated activation of AT2R, resulting in distinctive signaling outcomes including sodium excretion, inhibition of Na+,K+-ATPase, reductions in cyclic guanosine monophosphate (cGMP) levels, inhibition of particulate guanylate cyclase, and inhibition of catecholamine biosynthesis via decreased tyrosine hydroxylase activity. CGP42112 demonstrates neuroprotective effects in models of cerebral ischemia, and exerts antifibrotic and anti-inflammatory effects in cardiac tissue models. Initial confusion existed regarding its functional classification (antagonist vs. agonist), but subsequent studies confirmed its role as a full AT2R agonist. Though it has been widely used as a research tool, CGP42112's clinical development remains limited, with its main reported indications being cardiovascular disease models, hypertension research, and neuroprotection in ischemic stroke models[1][2][3][4][5][6][7][10].

Other names

CGP42112CGP-42112CGP 42112CGP42112ACGP-42112ACGP 42112A