TD-0212 is an orally active dual pharmacology antagonist of angiotensinIItype 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 angiotensinIItype 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 angiotensinIIreceptor agonist. In the renin-angiotensin system, angiotensin I is cleaved by the angiotensin-converting enzyme to form angiotensinII, which has effects on fluid and electrolyte, as well as homeostasis
FK-739 is an angiotensintype 1 receptor antagonist. FK 739 inhibits the specific binding of [125I]-angiotensinII to rat aortic smooth muscle cell membrane (IC50 = 8.6 nM) without displacing the specific binding of [125I]-angiotensinII to bovine cerebel
ZD 7155 hydrochloride is a potent and selective competitive antagonist for the angiotensinIItype 1 (AT1) receptor. It displaces [125I]-angiotensinII binding in guinea pig adrenal gland membranes with an IC50 value of 3.8 nM.
AngiotensinII is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensinII are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensinIItype 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 angiotensinIItype 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 angiotensinIItype 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 angiotensinIIreceptortype 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 angiotensinIItype 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 angiotensinIItype 1 (AT1) receptor antagonist valsartan. It is a degradation product formed under acidic conditions.