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).
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.
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.
Valsartan acid, a byproduct of the angiotensin II type 1 (AT1) receptor antagonist Valsartan, emerges through the activated sludge treatment process and has been identified as a contaminant in drinking water.