Losartan Carboxylic Acid

Cas No.:	124750-92-1
Chemical Name:	2-BUTYL-4-CHLORO-1-[(2'-(1-H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL)METHYL]-1-H-IMIDAZOLE-5-CARBOXYLIC ACID
Synonyms:	2-BUTYL-4-CHLORO-1-[(2'-(1-H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL)METHYL]-1-H-IMIDAZOLE-5-CARBOXYLIC ACID;LOSARTAN CARBOXY ACID;AKOS 91941;1h-imidazole-5-carboxylicacid,2-butyl-4-chloro-1-((2’-(14-tetrazol-5-yl)(1,1;e-3174;exp3174;l-158641;2-Butyl-4-chloro-1-[[2(1H-tetrazol-5-yl)[1,1biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylicAcid;2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid;EXP 317;EXP-3174;Losartan Carboxylic Acid;Losartan Carboxylic Acid NEW CATALOGUE NUMBER: see product L470510;1H-Imidazole-5-carboxylic acid,2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl);2-n-butyl-5-chloro-3-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid;E-3174, EXP-3174;2-Butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]imidazole-5-carboxylic acid
SMILES:	ClC(N=C(N1CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2)CCCC)=C1COC(O)=O
Formula:	C22H21ClN6O2
M.Wt:	436.89
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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].
In Vivo:	Losartan Carboxylic Acid (E-3174) (0.1 mg/kg; i.v. followed by 0.02 mg/kg/h for 5.5 h) induces a similar level of inhibition (87±4%) of the pressor responses to angiotensin I[3]. Intravenous Losartan Carboxylic Acid (0.1 mg/kg+0.01 mg/kg/min) is infused in anesthetized dogs with recent (8.1±0.4 days) anterior myocardial infarction. Electrolytic injury of the left circumflex coronary artery to induce thrombotic occlusion and posterolateral ischemia is initiated 1 h after the start of treatment[4]. Animal Model: Mongrel dogs of either sex, weighing 15-25 kg[3] Dosage: 0.1 mg/kg (followed by 0.02 mg/kg/h) Administration: i.v. for 5.5 hours Result: The pressor response was reduced by 87±4%.
In Vitro:	The specific binding of [125I]-angiotensin II to VSMC is inhibited by Losartan Carboxylic Acid (E-3174) with an IC50 of 1.1 nM. Losartan Carboxylic Acid abolishes the angiotensin II-induced formation of inositolphosphates in VSMC. Losartan Carboxylic Acid inhibits the angiotensin II-induced elevation of intracellular cytosolic Ca2+ concentration with an IC50 of 5 nM. Losartan Carboxylic Acid is more effective than losartan in blocking the angiotensin II-induced increase in Egr-1 mRNA. Losartan Carboxylic Acid inhibits the angiotensin II-induced cell protein synthesis with an IC50 of 3 nM[1].