Name | Losartan Potassium |
Synonyms | MK 954 Losartan Potassium LOSARTAN POTASSIUM LOSARTAN POTASSIUM SALT LOSARTAN MONOPOTASSIUM SALT 1h-imidazole-5-methanol,2-butyl-4-chloro-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphe 2-BUTYL-4-CHLORO-1-[[2'-(1H-TETRAZOL-5YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL potassium (2-butyl-4-chloro-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanolate potassium 5-(4'-{[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-yl]methyl}biphenyl-2-yl)tetrazol-1-ide 2-BUTYL-4-CHLORO-1-[[2'-(1H-TETRAZOLE-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL, POTASSIUM SALT 2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-methanol monopotassium salt |
CAS | 124750-99-8 |
EINECS | 200-287-4 |
InChI | InChI=1/C22H22ClN6O.K/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22;/h4-7,9-12H,2-3,8,13-14H2,1H3,(H,25,26,27,28);/q-1;+1 |
InChIKey | OXCMYAYHXIHQOA-UHFFFAOYSA-N |
Molecular Formula | C22H23ClKN6O |
Molar Mass | 462.01 |
Melting Point | 263-265°C |
Boling Point | 682°C at 760 mmHg |
Flash Point | 366.3°C |
Solubility | Soluble in water (>500 mg/ml), PBS (pH 7.2) (≥10 mg/ml), ethanol (≥20 mg/ml), DMSO (10 |
Vapor Presure | 1.55E-19mmHg at 25°C |
Appearance | White to yellowish powder |
Color | Off-white |
Merck | 14,5583 |
BRN | 5845770 |
Storage Condition | Inert atmosphere,Room Temperature |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
MDL | MFCD02092704 |
Use | A specific antagonist of the AT1 receptor with significant downstream effects. |
In vivo study | In monkeys with diet-induced hypercholesterolemia, Losartan(180 mg/day) caused a significant increase in plasma angiotensin II and angiotensin-(1-7). In monkeys with diet-induced hypercholesterolemia, Losartan(180 mg/day) reduced approximately 50% of the extent of fatty striae in the aorta, coronary arteries, and carotid arteries. In monkeys with diet-induced hypercholesterolemia, Losartan reduced the susceptibility to in vitro oxidation of low-density lipoprotein, serum levels of monocyte chemoattractant protein -1, and expression of circulating monocyte CD11b. In pregnant fbn1-apolipoprotein E-deficient mice, Losartan(5 mg/kg/day) caused a significant decrease in the development of atherosclerotic lesions. In apolipoprotein E-deficient mice, Losartan(5 mg/kg/day) significantly reduced the sensitivity of mouse LDL to fat oxidation after incubation in the presence of cuso4. In male Sprague Dawley rats, Losartan (10 mg/kg) administration increased angiotensin levels 4-to 6-fold without altering blood BK levels. In male Sprague Dawley rats, Losartan (10 mg/kg) increased plasma renin levels 100-fold and plasma angiotensin levels were reduced to 24% of controls without altering plasma aldisterol levels. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
WGK Germany | 3 |
RTECS | NI6755100 |
HS Code | 2933290000 |
white or off-white flowable crystalline powder. Very soluble in water, soluble in methanol or ethanol, slightly soluble in acetonitrile, methyl ethyl ketone and other general organic solvents, almost insoluble in chloroform.
2-butyl -4-chlorine 5-hydroxymethyl imidazole and sodium methoxide methanol solution stirring reaction, the formation of sodium salt and 4 '-bromomethyl-2-cyanobiphenyl in dimethylformamide, the obtained compound is etherified and then reacted with sodium azide in dimethylformamide containing ammonium chloride to obtain losartan by acidic hydrolysis.
Cozaar was first launched in 1994 and is currently approved in 93 countries for the treatment of hypertension. Oral administration of non-peptide angiotensin II receptor antagonists. Mainly used for primary hypertension. Cozaar is the first angiotensin II receptor antagonist (AIIA) class of antihypertensive drugs.