Angiotensin Receptor Agonist

Buloxibutid (AT2 receptor agonist C21) is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a K_i value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis.

AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC₅₀ of 21 nM.

TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R-β-arrestin-1-TRPC3-PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.

TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses^[1]

Angiotensin III, human, mouse is a heptapeptide, acts as an endogenous angiotensin type 2 receptor (AT₂R) agonist, with IC₅₀s of 0.648 nM and 21.1 nM for AT₂R and AT₁R, respectively.

TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses^[1]

Angiotensin II 5-valine is an agonist of angiotensin receptor.

(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β.

TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling. TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment.

Novokinin is a peptide agonist of the angiotensin AT2 receptor.

Aclerastide (DSC-127) is an angiotensin receptor agonist. Aclerastide also is a peptide analog of angiotensin II. Aclerastide can be used for the research of tissue regeneration in diabetic ulcers.

Angiotensin II (3-8), human (TFA) is a less effective agonist at the angiotensin AT₁ receptor.

L-162313 is a non-peptide angiotensin II AT1 and AT2 receptor agonist, with IC₅₀ values of 1.1 and 2.0 nM for AT1 and AT2 receptor, respectively. L-162313 can be used for the research of vasoconstriction, aldosterone release, and cardiovascular growth.

AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [¹²⁵I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC₅₀ of 21 nM.

(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a K_d of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes.

Sar-Arg-Val-Tyr-Val-His-NH2 is a G_q-biased agonists, exhibits 10-fold larger molecular efficacies at the AT₁R-Gq fusion protein compared with the AT₁R-βarr2 fusion protein.

Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca²⁺ levels. Angiotensin II also acts at the Na⁺/H⁺ exchanger in the proximal tubules of the kidney.

Novokinin TFA is a peptide agonist of the angiotensin AT2 receptor.

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.

Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca²⁺ levels. Angiotensin II also acts at the Na⁺/H⁺ exchanger in the proximal tubules of the kidney.