Losartan Carboxylic Acid

Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC) . Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].

Product Specifications

CAS Number

[124750-92-1]

Product Name Alternative

E-3174; EXP-3174

UNSPSC

12352005

Hazard Statement

H317, H360, H362

Target

Angiotensin Receptor; Drug Metabolite

Type

Reference compound

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/losartan-carboxylic-acid.html

Purity

99.47

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)O

Molecular Formula

C22H21ClN6O2

Molecular Weight

436.89

Precautions

H317, H360, H362

References & Citations

[1]Sachinidis A, et al. EXP3174, a metabolite of losartan (MK 954, DuP 753) is more potent than losartan in blockingthe angiotensin II-induced responses in vascular smooth muscle cells. J Hypertens. 1993 Feb;11 (2) :155-62.|[2]Inada Y, et al. Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors. Fundam Clin Pharmacol. 2002 Aug;16 (4) :317-23.|[3]Richard V, et al. Comparison of the effects of EXP3174, an angiotensin II antagonist and enalaprilat on myocardial infarct size in anaesthetized dogs. Br J Pharmacol. 1993 Nov;110 (3) :969-74.|[4]Lynch JJ Jr, et al. EXP3174, the AII antagonist human metabolite of losartan, but not losartan nor the angiotensin-converting enzyme inhibitor captopril, prevents the development of lethal ischemic ventricular arrhythmias in a canine model of recent myocardial infarction. J Am Coll Cardiol. 1999 Sep;34 (3) :876-84.