Home GPCR & G Protein Angiotensin Receptor

Angiotensin Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S1604 Olmesartan Medoxomil Olmesartan Medoxomil (CS-866,RNH-6270) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.
J Immunother Cancer, 2024, 12(11)e009805
Nan Fang Yi Ke Da Xue Xue Bao, 2020, 40(4):499-505
Sci Rep, 2015, 5:8116
Verified customer review of Olmesartan Medoxomil
S3057 Azilsartan Medoxomil Azilsartan Medoxomil (TAK-491) is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2.
J Immunother Cancer, 2024, 12(11)e009805
Acta Pharm Sin B, 2023, 13(2):662-677
Sci Rep, 2015, 5:8116
Verified customer review of Azilsartan Medoxomil
S8695 ML221 ML221 is a potent apelin receptor (APJ) functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor. The IC50 values of ML221 are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively.
Nat Commun, 2022, 13(1):4229
J Mol Cell Cardiol, 2021, S0022-2828(21)00246-7
Research Square, 2021, 10.21203/rs.3.rs-916525/v1
S5581 Olmesartan Olmesartan (RNH-6270) is an an angiotensin 2 receptor antagonist with antihypertensive activity.
J Immunother Cancer, 2024, 12(11)e009805
bioRxiv, 2020, 10.1101/2020.10.13.337774
E0039 A-779

A-779 is a potent and selective antagonist for Angiotensin-(1–7) (Ang-(1-7)) with an IC50 of 0.3 nM in a radioligand binding assay. This compound shows no significant affinity for AT1 or AT2 receptors at a concentration of 1 μM.
Int J Biol Sci, 2023, 19(8):2613-2629
Elife, 2022, 11e72266
S4975 Fimasartan Fimasartan (Kanarb) is a non-peptide angiotensin II receptor antagonist (ARB) with noncompetitive, insurmountable binding with the AT1 receptor. It is used for the treatment of hypertension and heart failure.
Drug Metab Dispos, 2020, 48(12):1264-1270
E4975 Angiotensin II human TFA Angiotensin II human TFA(DRVYIHPF TFA, Ang II TFA) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system that regulates blood pressure by activating AT1Rand AT2R, stimulating sympathetic activity, aldosterone production, and renal actions. It also promotes vascular cell growth, collagen synthesis, fibrosis, and induces apoptosis and capillary formation via a redox-sensitive pathway.
E1015 Angiotensin II human Angiotensin II human is a potent vasoconstrictor that induces angiogenesis by activating angiotensin II type 1 (AT1) receptor, which increases the production of vascular endothelial growth factor (VEGF) in a redox-sensitive manner and promotes the formation of capillaries from endothelial cells through the LOX-1-dependent redox-sensitive pathway.
S0326 Olodanrigan (EMA401) Olodanrigan (EMA401, PD-126055, (S) PD-126055) is a highly selective, orally active, peripherally restricted antagonist of angiotensin II type 2 receptor (AT2R). Its analgesic action appears to involve the inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
E4616 Buloxibutid Buloxibutid (AT2 Agonist C21) is a selective agonist of angiotensin II type 2 receptor (AT2R) with a Ki value of 0.4 nM for the AT2 receptor and a Ki >10 µM for the AT1 receptor. Its treatment significantly reduces vascular remodelling, improves hemodynamics, and decreases pulmonary collagen deposition in the Sugen-Hypoxia model of pulmonary hypertension.
S5980 Losartan Carboxylic Acid (EXP-3174) Losartan Carboxylic Acid (E-3174, EXP-3174), an active carboxylic acid metabolite of Losartan, is a non-peptide angiotensin II (AT1) receptor antagonist. This compound inhibits the specific binding of [125I]-angiotensin II to VSMC with IC50 of 1.1 nM.
E1060 AVE 0991 AVE 0991 is a potent, orally active, non-peptide selective agonist of the Mas receptor (MasR), functioning as a stable mimic of angiotensin-(1–7) [Ang-(1–7)]. It demonstrates high-affinity binding to endothelial MasR with an IC50 of 21 nmol/L in bovine aortic endothelial cell membranes and evokes endothelial effects similar to Ang-(1–7), including robust nitric oxide (NO) release with minimal superoxide (O2−) production.
E4951 Eprosartan Eprosartan (Teveten, SK-108566) is a selective, competitive, nonpeptide and orally active antagonist of angiotensin II receptor. This compound binds angiotensin II receptors with IC50 values of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively.
S7678 Sacubitril/valsartan (LCZ696) Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
Front Pharmacol, 2025, 16:1539032
J Immunother Cancer, 2024, 12(11)e009805
Ren Fail, 2024, 46(2):2392849
Verified customer review of Sacubitril/valsartan (LCZ696)
S6665 Sparsentan (PS-433540, RE-021) Sparsentan (PS-433540, RE-021, DARA) is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist.
Front Pharmacol, 2022, 13:964370
Biomedicines, 2021, 10(1)86