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| | Losartan carboxylic acid Basic information |
| Product Name: | Losartan carboxylic acid | | Synonyms: | AKOS 91941;2-BUTYL-4-CHLORO-1-[(2'-(1-H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL)METHYL]-1-H-IMIDAZOLE-5-CARBOXYLIC ACID;’-biphenyl)-4-yl)methyl)-;1h-imidazole-5-carboxylicacid,2-butyl-4-chloro-1-((2’-(14-tetrazol-5-yl)(1,1;1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-4-chloro-1H-imidazole-5-carboxylic acid;1H-Imidazole-5-carboxylicacid, 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-;2-Butyl-4-chloro-1-[[2(1H-tetrazol-5-yl)[1,1biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylicAcid;EXP 317 | | CAS: | 124750-92-1 | | MF: | C22H21ClN6O2 | | MW: | 436.89 | | EINECS: | 1592732-453-0 | | Product Categories: | Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals;Heterocycles | | Mol File: | 124750-92-1.mol |  |
| | Losartan carboxylic acid Chemical Properties |
| Melting point | 130-132°C | | Boiling point | 707.8±70.0 °C(Predicted) | | density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | Inert atmosphere,2-8°C | | 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 |
| Safety Statements | 24/25 | | HS Code | 29339900 |
| | Losartan carboxylic acid Usage And Synthesis |
| Description | Losartan carboxylic acid is a physiologically active metabolite of losartan , produced by cytochrome P450 isoforms in the liver. 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. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability. Losartan, but not its metabolite, inhibits platelet aggregation in vitro. | | Chemical Properties | Light-Yellow Solid | | Uses | Losartan carboxylic acid is used as 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. |
| | Losartan carboxylic acid Preparation Products And Raw materials |
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