Name | Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl] |
Synonyms | Ethyl Candesartan Candesartan ester Candesartan EP Imp A candesartan ethyl ester Candesartan Impurity 6 Candesartan Cilexetil EP Impurity A (Candesartan Ethyl Ester) Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl] Ethyl-2-Ethoxy-1-[[(2'-(1h-Tetrazol-5-Yl)Biphenyl-4-Yl)Methyl]Benzimidazole]-7-Carboxylate Ethyl 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-c Ethyl 1-((2-(2H-tetrazol-5-yl)-[1,1-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate 2-Ethoxy-1-[[2-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic Acid ethyl ester |
CAS | 139481-58-6 |
Molecular Formula | C26H24N6O3 |
Molar Mass | 468.51 |
Density | 1.33 |
Melting Point | 157-159°C |
Boling Point | 709.6±70.0 °C(Predicted) |
Flash Point | 382.928 °C |
Solubility | Chloroform (Slightly), Ethyl Acetate (Slightly, Sonicated), Methanol (Slightly) |
Appearance | Solid |
Color | White to Off-White |
pKa | 4.15±0.10(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Use | Intermediate |
candesartan | candesartan is rapidly hydrolyzed into the active metabolite candesartan in the body. candesartan is an angiotensin II receptor blocker. By binding to AT1 receptor, it inhibits the vasoconstriction of angiotensin II and the secretion of aldosterone, which weakens the renin-angiotensin activity and plays an anti-hypertensive effect. Clinically, it can be used to treat hypertension, left ventricular hypertrophy, congestive heart failure, myocardial infarction, hypertensive renal damage and diabetic nephropathy. This product is quickly absorbed after oral administration, and the blood concentration reaches a peak value 2 to 4 hours after taking the medicine. It takes effect 2 to 4 hours after oral administration, and reaches the maximum effect at 6 to 8 hours. Most patients showed curative effect within 2 weeks, and reached complete curative effect after 4 weeks. This medicine is difficult to penetrate the blood-brain barrier, but it can enter the fetus through the placental barrier. The half-life is 5.1~10.5 hours. |
candesartan cilexetil | candesartan cilexetil is an angiotensin II receptor antagonist developed by Takeda Pharmaceutical Company in Japan. It is clinically used to treat essential hypertension and congestive heart failure. Candesartan cilexetil is a prodrug that is absorbed by the gastrointestinal tract and hydrolyzed, so that only candesartan cilexetil in the serum, which is the active substance that blocks angiotensin II receptors. Take it once a day, the bioavailability is greater than 40%, and its blood pressure lowering effect lasts for 24 hours. It is mainly excreted from the body as a prototype, and only 15% is converted into inactive metabolites. Then the residual effect averaged 90%. However, the residual effect of the older angiotensin II antagonist losartan (Losartan) was 70% 24 hours after taking it. The examination and approval department requires that the residual effect should be at least 50% at the end of the taking interval. The long duration of action of this product may be due to its high affinity for the receptor. Compared with other antihypertensive drugs, low-dose candesartan cilexetil has the effect of lowering blood pressure. For example, the intensity of the hypotensive effect of 8 mg of candesartan cilexetil is similar to that of 5mg of amlodipine or 10mg of enalapril, and at least 50mg of losartan. |