Losartan carboxylic acid-d4 (hydrochloride)

• UNSPSC Description:

  Losartan carboxylic acid-d4 (hydrochloride) is deuterium labeled 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].

• Target Antigen:

  Angiotensin Receptor; Isotope-Labeled Compounds

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  GPCR/G Protein;Others

• Field of Research:

  Cardiovascular Disease

• Solubility:

  10 mM in DMSO

• Smiles:

  ClC1=C(C(O)=O)N(CC2=C([2H])C([2H])=C(C3=CC=CC=C3C4=NN=NN4)C([2H])=C2[2H])C(CCCC)=N1.Cl

• Molecular Weight:

  477.38

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.|[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]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.|[4]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.|[5]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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported