losartan

Losartan (DuP-753) is an angiotensin II receptor antagonist.

Losartan potassium (DuP-753 potassium), an Angiotensin II Receptor Blocker, selectively and competitively inhibits the binding of angiotensin II to the angiotensin I (AT1) receptor.

Losartan D4 Carboxylic Acid is the deuterium labeled Losartan, which is an angiotensin II receptor antagonist.

Losartan Carboxaldehyde is an endothelial cyclooxygenase (COX)-2 inhibitor.

Losartan D4 (DuP-753 D4) is a deuterated isotope of Losartan for isotopic tracing. Losartan is an angiotensin II receptor antagonist (IC50=20 nM).

Losartan potassium impurity E is a compound of Valsartan impurity.

Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.

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.

Trityllosartan is an intermediate in the preparation of Losartan.

UR-7247 is a novel orally active angiotensin II subtype I (AT1) antagonist, demonstrating very long pharmacological effects. in vivo studies indicate no significant difference between 10 mg UR-7247 and 100 mg losartan four hours post-administration, while in vitro blockade with 100 mg losartan exceeds that observed with UR-7247, confirming UR-7247’s extended plasma half-life potentially due to high-affinity protein binding, highlighting its long-lasting, well-tolerated AT1 receptor antagonism in healthy subjects.

Antihypertensive agent 2 (Compound 4g) effectively antagonizes angiotensin II receptor 1 and reduces blood pressure with potency equal to or greater than Losartan [1].