AT1 Receptor Antagonist

Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC₅₀ of 20 nM.

Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of ¹²⁵I-AngII to AT1 receptors with IC₅₀ of 9.2 nM.

DMP 811 is a potent, orally active and selective angiotensin II subtype receptor AT1 antagonist. DMP 811 exhibits selectivity for AT1 (IC₅₀ = 6 nM) over AT2 (IC₅₀ >10 μM). DMP 811 exhibits potent antihypertensive activity in rats and dogs. DMP 811 can be used for the research of hypertension.

Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research.

Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC₅₀ of 20 nM.

Angiotensin 1-7 (Ang-(1-7)) 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 inhibits purified canine ACE activity (IC₅₀=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .

Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.

A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.

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.

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.

CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.

Azilsartan medoxomil (TAK 491), a prodrug form of Azilsartan (HY-14914), is an orally active angiotensin II receptor type 1 antagonist. Azilsartan medoxomil can be used for the study of essential hypertension.

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.

Tasosartan is a long-acting angiotensin II (AngII) receptor antagonist.

BIBS 39 is a non-peptide angiotensin II receptor antagonist with antihypertensive activity, with higher affinity for the AT1 receptor than for the AT2 receptor. BIBS 39 competitively blocks AT1-mediated vasoconstriction and pressor responses, and effectively inhibits the activity of the renin-angiotensin-aldosterone system. BIBS 39 reduces diastolic blood pressure and induces mild, transient reflex tachycardia, with no off-target functional activity on the norepinephrine, K⁺/Cl⁻ or vasopressin pathways. BIBS 39 can be used in research related to hypertension and renal hypertension^[1][2][3].

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

Valsartan-d₉ is deuterium labeled valsartan. Valsartan is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research.

TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT₁) antagonist and neprilysin (NEP) inhibitor, with a pK_i of 8.9 for AT₁ and a pIC₅₀ of 9.2 for NEP.

Olmesartan methyl ester is an intermediate in the synthesis of Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor antagonist with IC₅₀ of 66.2 μM.

Olmesartan-d₆ (RNH-6270-d₆) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.