S5067 |
Losartan
|
Losartan(DuP-753) is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement. |
-
Eur J Med Res, 2024, 29(1):109
-
Proc Natl Acad Sci U S A, 2023, 120(6):e2219199120
-
Cell Death Discov, 2022, 8(1):134
|
|
S1578 |
Candesartan
|
Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM. |
-
Front Pharmacol, 2022, 13:828643
-
Hypertension, 2021, 77(5):1723-1736
-
Front Physiol, 2020-, Volume 11
|
|
S7098 |
PD123319
|
PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. |
-
Cell Res, 2021, 10.1038/s41422-020-00464-8
-
Int J Biochem Cell Biol, 2020, 121:105703
-
Neurosci Lett, 2020, 716:134684
|
|
S1359 |
Losartan Potassium
|
Losartan Potassium is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM. |
-
Int J Mol Sci, 2023, 24(4)3564
-
Drug Deliv Transl Res, 2023, 10.1007/s13346-023-01413-9
-
Adv Healthc Mater, 2021, e2001856
|
|
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.
|
-
Ren Fail, 2024, 46(2):2392849
-
Biomed Pharmacother, 2023, 162:114569
-
FEBS J, 2023, 290(8):2180-2198
|
|
S1738 |
Telmisartan
|
Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. |
-
Int Immunopharmacol, 2024, 139:112707
-
Exp Ther Med, 2022, 23(3):216
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
|
|
S1507 |
Irbesartan
|
Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM. |
-
Xenobiotica, 2020, 10.1080/00498254.2020.1745318
-
Front Physiol, 2019, 10:681
-
Antiviral Res, 2015, 120:140-6
|
|
S1894 |
Valsartan
|
Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure. |
-
Arch Toxicol, 2022, 96(4):1065-1074
-
Int J Mol Sci, 2021, 22(16)8598
-
Sci Rep, 2015, 5:8116
|
|
S2037 |
Candesartan Cilexetil
|
Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension. |
-
Int J Mol Sci, 2022, 23(20)12326
-
Sci Rep, 2015, 5:8116
-
Exp Biol Med, 2015, 10.1177/1535370215576312
|
|
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
-
Nat Commun, 2022, 13(1):4229
-
J Mol Cell Cardiol, 2021, S0022-2828(21)00246-7
|
|
S4102 |
Eprosartan Mesylate
|
Eprosartan(SKF-108566J) is a nonpeptide angiotensin II receptor antagonist, [3H]-eprosartan binds to the AT1 receptor with KD of 0.83 nM in rat vascular smooth muscle cells. |
-
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
-
bioRxiv, 2020, 10.1101/2020.10.13.337774
-
Sci Rep, 2016, 10.1038/srep25694
|
|
S3046 |
Azilsartan
|
Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM. |
-
Front Pharmacol, 2021, 12:774709
-
bioRxiv, 2020, 10.1101/2020.10.13.337774
-
Sci Rep, 2015, 5:8116
|
|
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. |
-
Nan Fang Yi Ke Da Xue Xue Bao, 2020, 40(4):499-505
-
Sci Rep, 2015, 5:8116
|
|
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
|
|
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. A-779 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
|
|
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. |
-
Sci Rep, 2015, 5:8116
|
|
S5581 |
Olmesartan
|
Olmesartan (RNH-6270) is an an angiotensin 2 receptor antagonist with antihypertensive activity. |
-
bioRxiv, 2020, 10.1101/2020.10.13.337774
|
|
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
|
|
E4975New |
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. |
|
|
E1015New |
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). Olodanrigan (EMA401) 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. |
|
|
E4616New |
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. Losartan Carboxylic Acid inhibits the specific binding of [125I]-angiotensin II to VSMC with IC50 of 1.1 nM. |
|
|
E4951New |
Eprosartan
|
Eprosartan(Teveten, SK-108566) is a selective, competitive, nonpeptide and orally active antagonist of angiotensin II receptor. Eprosartan binds angiotensin II receptors with IC50 values of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively. |
|
|
S5067 |
Losartan
|
Losartan(DuP-753) is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement. |
- Eur J Med Res, 2024, 29(1):109
- Proc Natl Acad Sci U S A, 2023, 120(6):e2219199120
- Cell Death Discov, 2022, 8(1):134
|
|
S1578 |
Candesartan
|
Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM. |
- Front Pharmacol, 2022, 13:828643
- Hypertension, 2021, 77(5):1723-1736
- Front Physiol, 2020-, Volume 11
|
|
S7098 |
PD123319
|
PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. |
- Cell Res, 2021, 10.1038/s41422-020-00464-8
- Int J Biochem Cell Biol, 2020, 121:105703
- Neurosci Lett, 2020, 716:134684
|
|
S1359 |
Losartan Potassium
|
Losartan Potassium is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM. |
- Int J Mol Sci, 2023, 24(4)3564
- Drug Deliv Transl Res, 2023, 10.1007/s13346-023-01413-9
- Adv Healthc Mater, 2021, e2001856
|
|
S1738 |
Telmisartan
|
Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. |
- Int Immunopharmacol, 2024, 139:112707
- Exp Ther Med, 2022, 23(3):216
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
|
|
S1507 |
Irbesartan
|
Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM. |
- Xenobiotica, 2020, 10.1080/00498254.2020.1745318
- Front Physiol, 2019, 10:681
- Antiviral Res, 2015, 120:140-6
|
|
S1894 |
Valsartan
|
Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure. |
- Arch Toxicol, 2022, 96(4):1065-1074
- Int J Mol Sci, 2021, 22(16)8598
- Sci Rep, 2015, 5:8116
|
|
S2037 |
Candesartan Cilexetil
|
Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension. |
- Int J Mol Sci, 2022, 23(20)12326
- Sci Rep, 2015, 5:8116
- Exp Biol Med, 2015, 10.1177/1535370215576312
|
|
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
- Nat Commun, 2022, 13(1):4229
- J Mol Cell Cardiol, 2021, S0022-2828(21)00246-7
|
|
S4102 |
Eprosartan Mesylate
|
Eprosartan(SKF-108566J) is a nonpeptide angiotensin II receptor antagonist, [3H]-eprosartan binds to the AT1 receptor with KD of 0.83 nM in rat vascular smooth muscle cells. |
- Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
- bioRxiv, 2020, 10.1101/2020.10.13.337774
- Sci Rep, 2016, 10.1038/srep25694
|
|
S3046 |
Azilsartan
|
Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM. |
- Front Pharmacol, 2021, 12:774709
- bioRxiv, 2020, 10.1101/2020.10.13.337774
- Sci Rep, 2015, 5:8116
|
|
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. |
- Nan Fang Yi Ke Da Xue Xue Bao, 2020, 40(4):499-505
- Sci Rep, 2015, 5:8116
|
|
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
|
|
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. A-779 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
|
|
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. |
- Sci Rep, 2015, 5:8116
|
|
S5581 |
Olmesartan
|
Olmesartan (RNH-6270) is an an angiotensin 2 receptor antagonist with antihypertensive activity. |
- bioRxiv, 2020, 10.1101/2020.10.13.337774
|
|
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
|
|
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). Olodanrigan (EMA401) 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. |
|
|
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. Losartan Carboxylic Acid inhibits the specific binding of [125I]-angiotensin II to VSMC with IC50 of 1.1 nM. |
|
|
E4951New |
Eprosartan
|
Eprosartan(Teveten, SK-108566) is a selective, competitive, nonpeptide and orally active antagonist of angiotensin II receptor. Eprosartan binds angiotensin II receptors with IC50 values of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively. |
|
|