TD-0212 is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).
TD-0212 TFA is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).
Angiotensin Fragment 1-7 is a type 1 angiotensin II receptor agonist. In the renin-angiotensin system, angiotensin I is cleaved by the angiotensin-converting enzyme to form angiotensin II, which has effects on fluid and electrolyte, as well as homeostasis
FK-739 is an angiotensin type 1 receptor antagonist. FK 739 inhibits the specific binding of [125I]-angiotensin II to rat aortic smooth muscle cell membrane (IC50 = 8.6 nM) without displacing the specific binding of [125I]-angiotensin II to bovine cerebel
ZD 7155 hydrochloride is a potent and selective competitive antagonist for the angiotensin II type 1 (AT1) receptor. It displaces [125I]-angiotensin II binding in guinea pig adrenal gland membranes with an IC50 value of 3.8 nM.
Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1) receptor. Losartan is a mammalian AT1 receptor antagonist with a Ki value of 5-20 nM. In humans, losartan effectively controls hypertension while protecting renal function. Nitric oxide (NO) causes vasodilation and also inhibits platelet and neutrophil aggregation in the endothelium. NO-losartan A possesses similar anti-hypertensive effects to losartan, with the addition of the vasodilating effects of NO release.
4-hydroxy Valsartan is a major metabolite of the angiotensin II type 1 (AT1) receptor antagonist valsartan . It reduces platelet aggregation induced by epinephrine and collagen but not ADP in human whole blood.
Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods.
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
TRV056 is a Gq-biased agonist of the angiotensin II type 1 receptor (AT1R), demonstrating efficacy in stimulating Gq-mediated cellular signaling. It can serve as a foundation for the development of Gq-biased AT1R agonists.
Desvaleryl valsartan is a potential impurity found in commercial preparations of the angiotensin II type 1 (AT1) receptor antagonist valsartan. It is a degradation product formed under acidic conditions.