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 99.98%
    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-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-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-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-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-P0205B
    Saralasin TFA
    		Antagonist 99.18%
    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-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-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-12765
    Losartan Carboxylic Acid
    		Antagonist 99.47%
    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 99.47%
    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-P1540
    Angiotensin III, human, mouse
    		Agonist 98.26%
    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-12405
    CGP-42112
    		Antagonist 99.84%
    CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
    CGP-42112
  • HY-116439
    Diisononyl phthalate
    		Activator 98.0%
    Diisononyl phthalate (DINP) is a phthalate used as a plasticizer. Diisononyl phthalate induces an increase in blood pressure through activation of the ACE/AT1R axis and inhibition of NO production in mice. Diisononyl phthalate can also be used in resin solvents, building materials, lubricants, adhesives, cosmetics and printing inks.
    Diisononyl phthalate
  • HY-B0780
    Fimasartan
    		Antagonist 99.60%
    Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1.
    Fimasartan
  • 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-P3136A
    TRV055 hydrochloride
    		Agonist 99.97%
    TRV055 (TRV120055) (hydrochloride) 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 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Angiotensin Receptor Isoform Comparison

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