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 theangiotensin-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 theangiotensinIItype 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 theangiotensinIItype 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 theangiotensinIItype 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. Theangiotensin 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 theangiotensinIIreceptortype 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 theangiotensinIItype 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 theangiotensinIItype 1 (AT1) receptor antagonist valsartan. It is a degradation product formed under acidic conditions.
L-163491 is a drug which acts as a partial agonist of angiotensinIIreceptortype 1, and with lower affinity as an agonist of angiotensinIIreceptortype 2, mimicking the action of angiotensinII. Its practical applications to date have been limited to scientific research into the function of theangiotensinreceptor system, but it has been suggested as a potential therapeutic agent for the treatment of inflammation of the lungs associated with certain viral diseases such as COVID-19.
AngiotensinII human TFA 是肾素-血管紧张素系统中的强效血管收缩剂,通过与 AT1R 和 AT2R 受体作用调节血压,可激活交感神经、促进醛固酮合成和肾功能,诱导血管平滑肌细胞增殖及成纤维细胞中 I 型和 III 型胶原合成,导致血管和心肌增厚、纤维化,并诱导凋亡及促进毛细血管生成,可用于构建心脏肥大、高血压和腹主动脉瘤模型。
Valsartan acid, a byproduct of theangiotensinIItype 1 (AT1) receptor antagonist Valsartan, emerges through the activated sludge treatment process and has been identified as a contaminant in drinking water.
TRV120027 is a β-arrestin-1-biased agonist of theangiotensinIIreceptortype 1. TRV120027 inhibits angiotensinII-mediated vasoconstriction and increases cardiomyocyte contractility.