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
-
UNIVERSITY OF PÉCS, 2023,
|
|
S1578 |
Candesartan
|
Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Front Pharmacol, 2022, 13:828643
-
Hypertension, 2021, 77(5):1723-1736
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Commun Biol, 2024, 7(1):1581
-
Int J Mol Sci, 2023, 24(4)3564
|
|
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.
|
-
J Immunother Cancer, 2024, 12(11)e009805
-
Ren Fail, 2024, 46(2):2392849
-
Biomed Pharmacother, 2023, 162:114569
|
|
S1738 |
Telmisartan
|
Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Int Immunopharmacol, 2024, 139:112707
-
Viruses, 2024, 16(10)1559
|
|
S1507 |
Irbesartan
|
Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Xenobiotica, 2020, 10.1080/00498254.2020.1745318
-
Front Physiol, 2019, 10:681
|
|
S1894 |
Valsartan
|
Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Arch Toxicol, 2022, 96(4):1065-1074
-
Int J Mol Sci, 2021, 22(16)8598
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Int J Mol Sci, 2022, 23(20)12326
-
Sci Rep, 2015, 5:8116
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
-
bioRxiv, 2020, 10.1101/2020.10.13.337774
|
|
S3046 |
Azilsartan
|
Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Front Pharmacol, 2021, 12:774709
-
bioRxiv, 2020, 10.1101/2020.10.13.337774
|
|
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
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Acta Pharm Sin B, 2023, 13(2):662-677
-
Sci Rep, 2015, 5:8116
|
|
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
|
|
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
|
|
E1015New |
Angiotensin II human
|
|
|
|
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. |
|
|
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
- UNIVERSITY OF PÉCS, 2023,
|
|
S1578 |
Candesartan
|
Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM. |
- J Immunother Cancer, 2024, 12(11)e009805
- Front Pharmacol, 2022, 13:828643
- Hypertension, 2021, 77(5):1723-1736
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Commun Biol, 2024, 7(1):1581
- Int J Mol Sci, 2023, 24(4)3564
|
|
S1738 |
Telmisartan
|
Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. |
- J Immunother Cancer, 2024, 12(11)e009805
- Int Immunopharmacol, 2024, 139:112707
- Viruses, 2024, 16(10)1559
|
|
S1507 |
Irbesartan
|
Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM. |
- J Immunother Cancer, 2024, 12(11)e009805
- Xenobiotica, 2020, 10.1080/00498254.2020.1745318
- Front Physiol, 2019, 10:681
|
|
S1894 |
Valsartan
|
Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure. |
- J Immunother Cancer, 2024, 12(11)e009805
- Arch Toxicol, 2022, 96(4):1065-1074
- Int J Mol Sci, 2021, 22(16)8598
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Int J Mol Sci, 2022, 23(20)12326
- Sci Rep, 2015, 5:8116
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
- bioRxiv, 2020, 10.1101/2020.10.13.337774
|
|
S3046 |
Azilsartan
|
Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM. |
- J Immunother Cancer, 2024, 12(11)e009805
- Front Pharmacol, 2021, 12:774709
- bioRxiv, 2020, 10.1101/2020.10.13.337774
|
|
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
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Acta Pharm Sin B, 2023, 13(2):662-677
- Sci Rep, 2015, 5:8116
|
|
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
|
|
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. |
|
|