Identification | Back Directory | [Name]
2-BUTYL-4-CHLORO-1-[(2'-(1-H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL)METHYL]-1-H-IMIDAZOLE-5-CARBOXYLIC ACID | [CAS]
124750-92-1 | [Synonyms]
e-3174 exp3174 EXP 317 l-158641 AKOS 91941 Losartan acid LOSARTAN CARBOXY ACID Losartan Carboxylic Acid ’-biphenyl)-4-yl)methyl)- EXP 3174 (LOSARTAN CARBOXYLIC ACID) Losartan Carboxylic AcidDiscontinued see product # L470510 Losartan Carboxylic Acid
NEW CATALOGUE NUMBER: see product # L470510 1h-imidazole-5-carboxylicacid,2-butyl-4-chloro-1-((2’-(14-tetrazol-5-yl)(1,1 2-Butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]imidazole-5-carboxylic acid 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic acid 2-Butyl-4-chloro-1-[[2(1H-tetrazol-5-yl)[1,1biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylicAcid 2-Butyl-3-[[2'-(2H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl]-5-chloro-3H-imidazole-4-carboxylic acid 1H-Imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)- 2-BUTYL-4-CHLORO-1-[(2'-(1-H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL)METHYL]-1-H-IMIDAZOLE-5-CARBOXYLIC ACID | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C22H21ClN6O2 | [MDL Number]
MFCD00871928 | [MOL File]
124750-92-1.mol | [Molecular Weight]
436.89 |
Chemical Properties | Back Directory | [Appearance]
Light-Yellow Solid | [Melting point ]
130-132°C | [Boiling point ]
707.8±70.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
Dimethylformamide, Dimethyl Sulfoxide, Methanol | [form ]
Solid | [pka]
0.79±0.50(Predicted) | [color ]
Light-Yellow | [InChIKey]
ZEUXAIYYDDCIRX-UHFFFAOYSA-N | [SMILES]
C1(CCCC)N(CC2=CC=C(C3=CC=CC=C3C3=NNN=N3)C=C2)C(C(O)=O)=C(Cl)N=1 |
Hazard Information | Back Directory | [Chemical Properties]
Light-Yellow Solid | [Usage]
A metabolite of Losartan | [Description]
Losartan carboxylic acid is a physiologically active metabolite of losartan (Item No. 10006594), produced by cytochrome P450 isoforms in the liver.1 Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.2,3,4 When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.4 However, the metabolite has very low oral bioavailability.4 Losartan, but not its metabolite, inhibits platelet aggregation in vitro.5 | [Uses]
A metabolite of Losartan | [Uses]
A metabolite of Losartan. | [Definition]
ChEBI: A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid. | [in vitro]
e-3174 potently blocked the specific binding of [125i]-aii to vsmc isolated from rat aorta. e-3174 was able to dampen the platelet-derived growth factor-induced increase in cell dna synthesis and protein, which led to the blockade of the aii-induced increase in cell protein [1]. | [in vivo]
rats were administrated e-3174 intravenously at a dose of l.0 mg/kg. after 6 hours, e-3174 markedly attenuated the cardiovascular effects of aii in rats. e-3174 induced a progressive fall in mean arterial pressure and a marked increase in renal flow only [2]. | [storage]
Store at -20°C | [References]
[1]. li, x. & widdop, r. angiotensin type i receptor antagonists cy-11974 and exp 3174 cause selective renal vasodilatation in conscious spontaneously hypertensive rats. clinical science, 1996; 91(2): 147-154. [2]. sachinidis, a., ko, y., weisser, p., zu bricbkwedde, m., dsing, r., & christian, r. et al. exp3174, a metabolite of losartan (mk954, dup753) is more potent than losartan in blocking the angiotensin ll-induced responses in vascular smooth muscle cells. journal of hypertension. 1993; 11(2): 155-162. |
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