at-1 receptor

ME-3221 is an angiotensin AT1 receptor antagonist that prevents hypertensive complications in aged stroke-prone hypertensive rats.

Pomisartan 2HCl (BIBR363 2HCL) is a small molecule AT1R antagonist used to study heart failure and hypertension.

Losartan potassium (DuP-753 potassium), an Angiotensin II Receptor Blocker, selectively and competitively inhibits the binding of angiotensin II to the angiotensin I (AT1) receptor.

Losartan (DuP-753) is an angiotensin II receptor antagonist.

Azilsartan (TAK-536) is an Angiotensin 2 Receptor Blocker that acts as an Angiotensin 2 Type 1 Receptor Antagonist, leading to a physiologic effect of decreased blood pressure.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

Eprosartan Mesylate (SKF-108566J) is a competitive and reversible Angiotensin II Receptor Blocker.

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.

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.

Candesartan (CV 11974) is an angiotensin II receptor blocker widely used in the treatment of hypertension and heart failure.

Eprosartan (SKF-108566J free base) is a selective, competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes, used as an antihypertensive agent. It exhibits inhibitory effects on angiotensin II receptors with IC50 values of 9.2 nM in rat adrenocortical membranes and 3.9 nM in human adrenocortical membranes.

Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.

L162389 is an orally active and potent angiotensin II receptor antagonist with a balanced affinity for AT1 and AT2 receptor subtypes that stimulates the conversion of phosphatidylinositol.

Olmesartan Medoxomil (Benicar) is an angiotensin II type 1 receptor blocker that is used to manage hypertension.

BIBS 39 is a novel nonpeptide angiotensin II (AII) receptor antagonist.

Angiotensin II (3-8), human (TFA), is an angiotensin AT1 receptor agonist with reduced activity.

A81988 is an antagonist of angiotensin AT1 receptors.

SL910102 is a nonpeptide angiotensin antagonist of the AT1 receptor.

KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. When labeled with the 11C isotope, KR31173 can be used as a tracer for positron emission tomography (PET). In mice, KR31173 exhibits favorable biodistribution and pharmacological characteristics. It selectively binds to organs in CD-1 mice known to have a high density of AT1 angiotensin receptors.

A 81282 is a selective antagonist of angiotensin receptors. It has the activity of lowering blood pressure.

GSK1820795A, a telmisartan analog, functions as a selective antagonist of hGPR132a, inhibiting the activation of yeast cells that express hGPR132a by N-acylamides [1]. Additionally, it acts as an angiotensin II antagonist and a partial PPARγ agonist (compound 38) [2].

α1 adrenoceptor-MO-1 (S enantiomer) has affinity at alpha 1 adrenergic receptor with alphalytic activity and analgesic action. It has more active than R enantiomer.

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.