Drug intelligence / Profile preview

PD123319

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Intra-arterial, Intracerebroventricular, Subcutaneous
01

Overview

PD123319 is a synthetic, non-peptide small molecule that functions primarily as a selective antagonist of the angiotensin II type 2 receptor (AT2R). It is widely used in research to investigate the roles of the renin-angiotensin system, particularly in studies involving vascular contraction, inflammation, and organ fibrosis. PD123319 exhibits potent inhibition of Ang II binding to the AT2 receptor with reported in vitro IC50 values around 34 nM, and is much less potent at the angiotensin II type 1 receptor (AT1R). In animal models, PD123319 has been found to attenuate inflammation, oxidative stress, and pathophysiological changes in cardiovascular and gastrointestinal tissues induced by angiotensin II. Some evidence suggests PD123319 can have effects partially independent from its AT2 receptor blockade, especially in vivo. It is not approved for clinical use and is used exclusively as a pharmacological tool in preclinical and academic research[1][2][4][7][8].

Other names
PD123319 ditrifluoroacetatePD-123319 ditrifluoroacetatePD 123319 ditrifluoroacetate
02

Targets

AGTR1 (Angiotensin II Type-1 receptor)AGTR2 (AT2)

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