Fimasartan(CAS NO.:247257-48-3)
Basic information
Product Name: Fimasartan
Synonyms:
CAS: 247257-48-3
MF: C27H31N7OS
MW: 501.65
Chemical Properties
Boiling Point: 693.0±65.0 °C(Predicted)
Density: 1.25
storage temp: 2-8°C
Solubility: DMSO (Slightly), Methanol (Slightly)
Form: Solid
Pka: 4.16±0.10(Predicted)
Color: White to Off-White
InChI: NA
InChIKey: NA
SMILES: NA
product description
It was developed by Boryeong Pharmaceutical in South Korea under the chemical name of 2-butyl-5-dimethylaminothiocarbamoylmethyl-6-methyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methylpyrimidine-4(3H)-one. As the latest generation of ARBs, femarsartan has demonstrated rapid and effective antihypertensive effects in a variety of hypertension types, and has shown a more effective antihypertensive effect than other ARBs such as losartan and olmesartan cille.
Pharmacological studies have shown that femarsartan can competitively sever the binding of angiotensin II to AT1 receptors in the human gastrointestinal tract and plasma, thereby lowering blood pressure. Experiments conducted in hypertensive rats and canine models of nephrogenic hypertension have shown that the antihypertensive effect of non-marsartan is enhanced with increasing dose, and its affinity for AT1 receptor is 10,000 times stronger than that of AT2. Femasartan is more effective than olmesartan in lowering diastolic blood pressure in the heart.
Non-marsartan is well tolerated, the safety is higher than that of other ARB drugs, and long-term use has a good protective effect on heart and kidney function. It is excreted mainly through feces and bile, with less than 3% of urine excretion after 24 hours of medication, and is metabolized mainly by CYP3A. There is no interaction with hydrochlorothiazide, digoxin, amlodipine and warfarin. Clinical trials have shown that femarsartan has a good antihypertensive effect, and its efficacy is better than losartan and valsartan. Femarsartan can be used in patients with mild hepatic impairment but not in patients with moderate or severe hepatic impairment.
The marketing of femarsartan provides a new treatment for the treatment of hypertension, but because it is new to the market, there is insufficient data on its efficacy and safety, so more extensive research is urgently needed. The molecular formula of non-masartan is C27H31N7OS, the molecular weight is 501.65, and the purity is ≥ 98%. The storage conditions are that the powder is stored at -25~-15 °C, and the validity period is 3 years; When soluble in solvent, store at -85~-65 °C, valid for 2 years. It should be used safely, avoid inhalation, swallowing or direct contact with skin and eyes, and only use it for scientific research purposes, and prohibit it from being used on the human body.