2. Signaling Pathways
  3. GPCR/G Protein
  4. Angiotensin Receptor

Angiotensin Receptor

Angiotensin Receptor

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Angiotensin receptors are a class of G protein-coupled receptors with angiotensin II as their ligands. They are important in the renin-angiotensin system: they are responsible for the signal transduction of the vasoconstricting stimulus of the main effector hormone, angiotensin II. The AT1 and AT2 receptors have a similar affinity for angiotensin II, which is their main ligand. The AT1 receptor is the best elucidated angiotensin receptor. AT2 receptors are more plentiful in the fetus and neonate. Other poorly characterized subtypes include the AT3 and AT4 receptors.

Angiotensin Receptor Isoform Specific Products:

Angiotensin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15778
    AVE 0991
    		Agonist 99.91%
    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
    AVE 0991
  • HY-15477
    YS-49
    		Inhibitor 99.80%
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
    YS-49
  • HY-10259A
    PD 123319 ditrifluoroacetate
    		Antagonist 99.82%
    PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
    PD 123319 ditrifluoroacetate
  • HY-17005
    Olmesartan medoxomil
    		Inhibitor 99.12%
    Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
    Olmesartan medoxomil
  • HY-17621
    Sparsentan
    		Antagonist 99.77%
    Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
    Sparsentan
  • HY-13106
    Olodanrigan
    		Antagonist 98.89%
    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
    Olodanrigan
  • HY-P2141
    TRV-120027
    		Agonist 98.11%
    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.
    TRV-120027
  • HY-P3108
    Alamandine
    		Inhibitor 98.86%
    Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions.
    Alamandine
  • HY-P0205B
    Saralasin TFA
    		Antagonist 99.65%
    Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.
    Saralasin TFA
  • HY-14914
    Azilsartan
    		Antagonist 99.68%
    Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research.
    Azilsartan
  • HY-14736
    Azilsartan medoxomil
    		Antagonist 99.60%
    Azilsartan medoxomil (TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
    Azilsartan medoxomil
  • HY-12403A
    Talfirastide acetate
    		Antagonist 99.77%
    Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium.
    Talfirastide acetate
  • HY-P1540
    Angiotensin III, human, mouse
    		Agonist 98.27%
    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.
    Angiotensin III, human, mouse
  • HY-B0935
    Benzyl benzoate
    		Inhibitor 99.94%
    Benzyl benzoate (Phenylmethyl benzoate) is an orally active anti-scabies agent, acaricide (EC50= 0.06 g/m2) and fungicide. Benzyl benzoate is an angiotensin II (Ang II) inhibitor with antihypertensive effects. Benzyl benzoate can be used in perfumes, pharmaceuticals and the food industry.
    Benzyl benzoate
  • HY-12765
    Losartan Carboxylic Acid
    		Antagonist 99.26%
    Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
    Losartan Carboxylic Acid
  • HY-P3136
    TRV055
    		Agonist 99.75%
    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]
    TRV055
  • HY-12405
    CGP-42112
    		Antagonist 99.84%
    CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
    CGP-42112
  • HY-P0108
    Angiotensin II 5-valine
    		Agonist 99.66%
    Angiotensin II 5-valine is an agonist of angiotensin receptor.
    Angiotensin II 5-valine
  • HY-P2141A
    TRV-120027 TFA
    		Agonist 99.69%
    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.
    TRV-120027 TFA
  • HY-13948B
    Angiotensin II human TFA
    		Modulator 98.84%
    Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human TFA induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human TFA also induces apoptosis. Angiotensin II human TFA induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
    Angiotensin II human TFA
Cat. No. Product Name / Synonyms Application Reactivity
Angiotensin Receptor Isoform Comparison

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