AT2 Receptor Antagonist

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

PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 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.

Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

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

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].

L-161638 is a potent, selective and orally active AT2 receptor antagonist. L-161638 can be used for the research of cardiovascular disease, such as hypertension.

PD 123177 is a nonpeptide antagonist specific for angiotensin II (AII) subtype AT2 receptor in mammalian systems.

Candesartan methyl ester (compound 14) is an antagonist for angiotensin II (AII) receptor with an IC₅₀ of 66 nM. Candesartan methyl ester exhibits blood pressure lowering activity in rats models.

PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 nM.

Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

Ripisartan (UP-2696) is an angiotensin II receptor antagonist. Ripisartan is orally available. Ripisartan binds to angiotensin II receptors, dilates blood vessels, and lowers blood pressure.

AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a K_i of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.

AT2R antagonist 2 (compound I-16) is an orally active AT2R antagonist.

L-163958 is an efficient, orally active, balanced angiotensin II receptor (AII receptor) antagonist. L-163958 has balanced high affinity for AT1 and AT2, with its IC₅₀ values being 0.16, 0.12, 0.50, and 0.64 nM in rabbit aorta (AT1), rat midbrain (AT2), human adrenal gland (AT1), and human adrenal gland (AT2), respectively. L-163958 has a strong inhibitory effect on the pressor activity in rats. L-163958 can be used for the study of hypertension and related cardiovascular diseases.

TA-606 is a potent and orally active angiotensin II-receptor antagonist. TA-606 shows antihypertensive efficacy. TA-606 can be used for hypertension research.

rac-Olodanrigan (rac-EMA401; EMA400) is a racemic mixture of the S-enantiomer (EMA401; HY-13106) and R-enantiomer (EMA402). rac-Olodanrigan is a potent and selective AT₂ receptor antagonist with IC₅₀s of 75.2 nM and 2918 nM for AT₂R and AT₁R, respectively. rac-Olodanrigan evokes dose-dependent relief of mechanical allodynia in the ipsilateral hind paws of rats with a chronic constriction injury (CCI) of the sciatic nerve.

CL-329167 (compound 12) is an orally active and competitive angiotensin II receptor antagonist (IC₅₀=6 nM). CL-329167 can be used in the research of hypertension.