AT1R-agonist-1 

AT1R-agonist-1 is an angiotensin II type 1 receptor (AT1R) agonist with a K_i value of 1.4 nM. AT1R-agonist-1 exhibits low Gαq activity, retains β-arrestin recruitment function, and accesses the deep allosteric pocket inside AT1R via its flexible side chain. AT1R-agonist-1 possesses positive inotropic effects (enhancing cardiac contractile function) and causes almost no increase in blood pressure. AT1R-agonist-1 can be used for research on conditions such as refractory cardiogenic shock^[1].

AT1R-agonist-1 (Compound 12) (10 μM; 10 min) acts as a highly weak partial agonist of Gαq signaling in AT1R-expressing HEK293 cells, with an EC₅₀ > 10,000 nM and 11% relative efficacy to AngII^[1].
AT1R-agonist-1 (dose-response concentrations, 10 μM; 10 min) potently recruits β-arrestin2 to AT1R in HEK293 cells, with an EC₅₀ of 2.5 nM and 89% relative efficacy to AngII^[1].
AT1R-agonist-1 (dose-response concentrations, 10 μM; 10 min) acts as a partial agonist of PKC signaling in AT1R-expressing HEK293 cells, with an EC₅₀ of 4.8 nM and 51% relative efficacy to AngII^[1].
AT1R-agonist-1 (dose-response concentrations, 10 μM; 3 min) acts as a partial agonist of Rho signaling in Gα₁₂/₁₃-knockout, AT1R-expressing HEK293 cells, with an EC₅₀ of 21 nM and 47% relative efficacy to AngII^[1].
AT1R-agonist-1 (10 μM; 1 min) shows negligible PKC activation in rat primary VSMCs, with an EC₅₀ >10,000 nM and 13% relative efficacy to AngII^[1].
AT1R-agonist-1 (10 μM; 1 min 30 s) shows negligible Rho activation in rat primary VSMCs, with an EC₅₀ >10,000 nM and 12% relative efficacy to AngII^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AT1R-agonist-1 (Compound 12) (0.96-9.6 nmol/kg/min; intravenous injection; continuous infusion; 10 min) enhances left ventricular ejection fraction in normotensive male Sprague-Dawley rats, while only inducing a mild, transient pressor response^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1152.30

C₅₇H₇₇N₁₃O₁₃

3124030-35-6

Asp-Arg-Val-Tyr-Ile-His-Pro-{Tyr(Bzl)}

DRVYIHP-{Tyr(Bzl)}

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hadjadj M, et al. Tunable Biased Signaling of the Angiotensin II Type 1 Receptor for Inotropy C-Terminal Peptide Engineering and Allosteric Site Targeting. Journal of medicinal chemistry. 2026 Feb 12;69(3):2063-2081.  [Content Brief]