Cardiovascular drugs Uses Category Toxicity grading Acute toxicity Flammability hazard characteristics Storage Characteristics Extinguishing agent
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Bisoprolol

Cardiovascular drugs Uses Category Toxicity grading Acute toxicity Flammability hazard characteristics Storage Characteristics Extinguishing agent
Bisoprolol Structure
Bisoprolol
  • CAS No.66722-44-9
  • Chemical Name:Bisoprolol
  • CBNumber:CB8245445
  • Molecular Formula:C18H31NO4
  • Formula Weight:325.44
  • MOL File:66722-44-9.mol
Bisoprolol Property
  • Melting point 100 °C
  • Boiling point 445.0±45.0 °C(Predicted)
  • Density 1.033±0.06 g/cm3(Predicted)
  • storage temp. -20°C Freezer, Under Inert Atmosphere
  • solubility Chloroform (Sparingly), Methanol (Slightly)
  • pka pKa 9.57(H2O(extrap) t=25±1 Iunde?ned Aratmosphere) (Uncertain)
  • form Liquid (Density: 1.033±0.06 g/cm3)
  • color Yellow
  • Water Solubility 5.5ug/L(100 ºC)
  • CAS DataBase Reference 66722-44-9(CAS DataBase Reference)
  • FDA UNII Y41JS2NL6U
  • ATC code C07AB07
  • NIST Chemistry Reference Bisoprolol(66722-44-9)
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H362
  • Precautionary statements P202-P263-P264-P270-P301+P312-P308+P313
Bisoprolol Price More Price(1)
  • Brand: Sigma-Aldrich(India)
  • Product number: 50787
  • Product name : Bisoprolol
  • Purity: analytical standard
  • Packaging: 25MG
  • Price: ₹12935.88
  • Updated: 2022/06/14
  • Buy: Buy

Bisoprolol Chemical Properties,Usage,Production

  • Cardiovascular drugs Bisoprolol is successfully developed by the German Merck in 1978, in the world ,it is already the drug of choice on clinicalcommonly used to treat hypertension, angina, arrhythmias and heart failure and other cardiovascular diseases, the product is highly selective β1-adrenergic receptor blocker,it has hydrophilic and lipophilic properties,it has no intrinsic sympathomimetic activity and membrane stability, and its negative inotropic effect is weaker.It has two β receptor binding sites with ultra-high affinity and high affinity ,its drug action is extremely powerful,it is 7 to 10 times stronger than atenolol and metoprolol . It has highly β1 receptor selectivity, selective research about model complex β1/β2 finds out that: propranolol is 1/3,atenolol is 20/1 , bisoprolol is 60/1. Another study compares the β1/β2 selectivity of metoprolol and bisoprolol, the results show that the former is 74/1,the latter is 119/1. Like other β-blockers, bisoprolol by blocking heartβ1 receptors, and inhibiting the renin-angiotensin system, plays a role in the treatment of hypertension, angina, arrhythmia. Recent studies indicate that substance P has effect on dilating the blood vessels to reduce the role of peripheral resistance, content of substance P in patients with hypertension decreases significantly,there is a significant rebound of substance P while there is a decrease in blood pressure after the treatment of bisoprolol, which may be one of the possible mechanisms of antihypertension . Another study shows that bisoprolol can not only decrease the blood pressure, but can also improve diastolic function; it has no adverse effects on blood sugar, blood lipids , conclusion in diabetics is also like this . It is mainly used to treat supraventricular tachycardia, atrial fibrillation, ventricular premature contraction, coronary heart disease, angina, mild to moderate hypertension, it is also used in heart failure caused by dilated cardiomyopathy and ischemic heart disease.
    Oral F is up to 88%. Tmax is 1.5~3 h. PPB is 30%. Plasma clearance T1/2 is 10~12 h. The one dose effect can be maintained for 24 h. Because its hydrophilic character is equal to lipophilic character, its adverse reactions on central nervous system are lighter than metoprolol with lipophilic character,and its adverse reactions on renal function is smaller compared withatenolol with hydrophilic character . Bisoprolol have two equal clearance ways ,half of it is metabolized to the non-active substances in the liver , the other half is excreted in the form of the prototype by the kidneys. [Note and taboos]it is similar to atenolol.
    The above information is edited by the chemicalbook of Tian Ye.
  • Uses It is used for the treatment of cardiovascular and cerebrovascular diseases.
  • Category Toxic Substances
  • Toxicity grading Middle toxic
  • Acute toxicity Intravenous-Mouse LD50: 164 mg/kg.
  • Flammability hazard characteristics Combustible; combustion produces toxic nitrogen oxide gases.
  • Storage Characteristics Ventilated, low-temperature ,dry storeroom.
  • Extinguishing agent Water, dry powder, foam, sand.
  • Chemical Properties Yellow Oil
  • Uses A selective a-adrenergic blocker. Used as an antihypertensive
  • Uses Cardensiel is an intermediate in the synthesis of 3,3''-(Isopropylazanediyl)bis(1-(4-((2-isopropoxyethoxy)methyl)phenoxy)propan-2-ol) (I824005), which is an impurtiy of Bisoprolol (B510500), a selective β-adrenergic blocker. Used as an antihypertensive.
  • Definition ChEBI: Bisoprolol is a secondary alcohol and a secondary amine. It has a role as an antihypertensive agent, a beta-adrenergic antagonist, an anti-arrhythmia drug and a sympatholytic agent.
  • in vivo

    Bisoprolol (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2].
    Bisoprolol (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
    Bisoprolol (oral gavage, 1 mg/kg, daily for 6 weeks) reverses small conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model[5].

    Animal Model:Ischemia/reperfusion (I/R) injury rats[2]
    Dosage:0.5, 5, 10 mg/kg
    Administration:Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion.
    Result:Reduced infarct size from 44% in I/R group to 31% in treated group.
    Animal Model:Cadmium-induced rats[4]
    Dosage:2, 8 mg/kg
    Administration:Oral gavage, daily for four weeks.
    Result:Decreased mean arterial pressure (MAP) at 8 mg/kg.
    Decreased serum biomarkers (ALT, AST) and NF-kB p65 expression and TNF-α levels (cardiac tissue samples) at 8 mg/kg.
  • Enzyme inhibitor This oral cardiospecific β-blocker (FWfree-base = 325.45 g/mol; CAS 66722- 44-9; IUPAC: (RS)-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-3- (isopropylamino)propan-2-ol), also named Zebeta? (oral tablets as fumarate salt), selectively targets β1-adrenergic receptors, blocking epinephrine stimulation of β1-adrenoreceptors that are concentrated in the heart muscle cells and heart conduction tissue as well as kidney juxtaglomerular cells. Bisoprolol is used to treat hypertension, coronary heart disease, arrhythmias, ischemic heart diseases, and myocardial infarction after the acute event. Given such versatility, bisoprolol is understandably included in the World Health Organization's List of Essential Medicines. Pharmacokinetics: Bioavailability > 90%; Hepatic metabolism (50%) by CYP2D6 and CYP3A4; Biological t1/2 = 10-12 hours.
  • IC 50 Beta-1 adrenergic receptor
Bisoprolol Preparation Products And Raw materials
Raw materials
Preparation Products
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Bisoprolol Spectrum
66722-44-9, BisoprololRelated Search:
  • Pharmaceuticals
  • Isotope Labeled Compounds
  • Intermediates & Fine Chemicals
  • API
  • Isotope Labelled Compounds
  • 杂质对照品
  • WHO基本药物配体
  • 定制产品
  • 原料药
  • 天然产物
  • 医药中间体
  • C18H26NO4D5
  • C18H26D5NO4
  • C18H31NO4
  • 86426-27-3
  • 甲醇中比索洛尔
  • 比索洛尔-D5 半富马酸
  • 比索洛尔相关杂质
  • 1-{4-[(2-异丙氧基乙氧基)甲基]苯氧基}-3-(异丙基氨基)-2-丙醇
  • 比索洛尔-D5半富马酸盐
  • 比索洛尔杂质F
  • 比索洛尔杂质H
  • 比索洛尔杂质I
  • 比索洛尔杂质O
  • 比索洛尔杂质P
  • 比索洛尔 标准品
  • 比索洛尔-D5半富马酸酯
  • 化合物BISOPROLOL
  • 比索洛尔 API和各步中间体
  • 1-[4-[2-(1-甲基乙氧基)乙氧基]甲基]苯氧基-3-[(1-甲基乙基)胺基]-2-丙醇
  • 1-{4-[(2-异丙氧基乙氧基)甲基]苯氧基}-3-(异丙基氨基)-2-丙醇反丁烯二酸盐
  • 比索洛尔溶液, 100PPM
  • 1-[4-[[2-(1-甲基乙氧基)乙氧基]甲基]苯氧基]-3-[(1-甲基乙基)氨基]-2-丙醇
  • 比索洛尔
  • 66722-44-9
  • Trimethoprim Impurity 52
  • Bisoprolol in Methanol
  • (RS)-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-3-(isopropylamino)propan-2-ol
  • Cardensiel
  • Bisoprolol base
  • Bisoprolo
  • 1-(4-((2-isopropoxyethoxy)Methyl)phenoxy)-3-(isopropylaMino)propan-2-ol
  • Bisoprolol-d5 HeMifuMarate
  • Bisolo
  • 1-(propan-2-ylamino)-3-[2-(1-propan-2-yloxyethoxymethyl)phenoxy]-2-propanol
  • Bisoprolol USP/EP/BP
  • 1-[isopropylamino]-3-[isopropoxyethoxymethylphenoxy]-2-propa...
  • BisoprololQ: What is Bisoprolol Q: What is the CAS Number of Bisoprolol Q: What is the storage condition of Bisoprolol Q: What are the applications of Bisoprolol
  • Bisoprolol D5 FumarateQ: What is Bisoprolol D5 Fumarate Q: What is the CAS Number of Bisoprolol D5 Fumarate Q: What is the storage condition of Bisoprolol D5 Fumarate Q: What are the applications of Bisoprolol D5 Fumarate
  • 66722-44-9 Bisoprolol
  • Racemic Bisoprolol
  • 1-(p-2-Isopropoxyethoxymethylphenoxy)-3-isopropylaminopropan-2-ol
  • (S)-1-[(1-Methylethyl)amino]-3-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-2-propanol
  • (S)-1-(Isopropylamino)-3-[4-[(2-isopropoxyethoxy)methyl]phenoxy]-2-propanol
  • (S)-1-(Isopropylamino)-3-[4-(2-isopropoxyethoxymethyl)phenoxy]-2-propanol
  • 1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol-d5
  • Bisoprolol-D5
  • 1-[4-[2-(1-Methylethoxy)ethoxymethyl]phenoxy]-3-(1-methylethylamino)propan-2-ol

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