ChemicalBook
Chinese english Germany Japanese Korea

Bosentan Produkt Beschreibung

Bosentan Struktur
147536-97-8
CAS-Nr.
147536-97-8
Englisch Name:
Bosentan
Synonyma:
BOSENTAN;Actelion;ro47-0203;Bosentan 13C6;ro47-0203/039;Bosentan impurity;bosentan , CID 104865;Bosentan (Benzenesulfonamide);2’-bipyrimidin)-4-yl)-enoxy)(;Bosentan, 99%, a endothelin (ET) receptor antagonist
CBNumber:
CB3425624
Summenformel:
C27H29N5O6S
Molgewicht:
551.61
MOL-Datei:
147536-97-8.mol

Bosentan Eigenschaften

Schmelzpunkt:
107-110°C
storage temp. 
-20°C Freezer
CAS Datenbank
147536-97-8(CAS DataBase Reference)

Sicherheit

HS Code  29350090

Bosentan Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Bosentan was introduced in the US as a twice-daily oral treatment for pulmonary arterial hypertension. It can be synthesized in five steps via condensation of diethyl (2- methoxyphenoxy)malonate with pyrimidine-2-carboxamidine to give the precursor of the symmetrical central dichloropyrimidine ring which is then successively treated with the potassium salt of 4-tert-butylbenzenesulfonamide and the sodium salt of ethylene gycol. Bosentan is the first endothelin (ET) receptor antagonist to be launched. ET-1, the most potent endogenous vasoconstrictor known, has been demonstrated to play a major role in the functional and structural changes observed in pulmonary hypertension. Bosentan is a mixed ETA and ETB receptor antagonist that inhibits the pulmonary arterial vasoconstricting effect of ET-1 predominantly mediated via ETA receptors on smooth muscle cells. In a hypoxia-induced model of pulmonary hypertension in rat, it reduced the development of pulmonary hypertension as well as right ventricular hypertrophy and prevented pulmonary arterial remodeling. In clinical trials, patients treated with bosentan showed a 20% increase in exercise capacity compared to placebo as measured by the six minute walk test. Bosentan not only improved the distance walked by patients but also significantly decreased mean pulmonary artery pressure, mean pulmonary vascular resistance, mean capillary wedge pressure and mean right atrial pressure. It demonstrated a beneficial selectivity for the pulmonary vasculature since it had no significant effect on mean aortic blood pressure and systolic vascular resistance. The compound is hepatically metabolized into three major metabolites by CYP3A4 and 2C9 and almost exclusively eliminated in the bile. Although large interspecies differences in systemic plasma clearance was observed (1.5 mL/min/kg in dogs to 72 mL/min/kg in rabbits), a satisfactory systemic clearance (2 mL/min/kg) was measured in human. The most frequent adverse effect was reversible elevation of liver transaminases. This adverse reaction appears to be due to intracellular accumulation of cytotoxic bile salts resulting from inhibition of the hepatocanalicular bile salt export pump by bosentan.

Chemische Eigenschaften

Pale Yellow to Off-White Solid

Originator

Roche (Switzerland)

Verwenden

A mixed endothelin receptor antagonist. Used as a vasodilator. Antihypertensive.

Trademarks

Tracleer (Actelion).

Allgemeine Beschreibung

Bosentan, N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]-4-tertbutyl-benzenesulfonamide (Tracleer, Bozentan), was thefirst endothelin receptor antagonist marketed in the UnitedStates. Bosentan works by competitively blocking the endothelinreceptor subtypes ETA and ETB. In binding to thereceptors, it blocks the effects of endothelin, which includeconstriction of the vascular smooth muscle, which leads tonarrowing of the blood vessels and hypertension. Althoughit is not selective for the ETA receptors, it does have a higheraffinity for that subtype over ETB. However, the clinical significanceof selectivity over preferential receptor bindinghas not been demonstrated. Bosentan is an inducer ofCYP2C9 and CYP3A4, and patients using bosentan must bemonitored for liver toxicity.

Hazard

A reproductive hazard.

Bosentan Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Bosentan Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 153)Lieferanten
Firmenname Telefon Fax E-Mail Land Produktkatalog Edge Rate
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19918 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21752 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32447 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2543 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30002 58
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23976 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 sales@jushengtech.com CHINA 28236 58
Hubei xin bonus chemical co. LTD
86-13657291602
027-59338440 sales@guangaobio.com CHINA 23049 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58

147536-97-8()Verwandte Suche:


  • Bosentan 13C6
  • 4-(tert-Butyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulf
  • Bosentan impurity
  • Bosentan (Benzenesulfonamide)
  • bosentan , CID 104865
  • Bosentan, 99%, a endothelin (ET) receptor antagonist
  • 2’-bipyrimidin)-4-yl)-enoxy)(
  • benzenesulfonamide,4-(1,1-dimethylethyl)-n-(6-(2-hydroxyethoxy)-5-(2-methoxyph
  • ro47-0203
  • ro47-0203/039
  • BOSENTAN
  • Ro-47-0203, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2bipyrimidin]-4-yl]benzenesulfonamide
  • p-tert-Butyl-N-[6-(2-hydroxyethoxy)-5-(o-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide
  • 4-TERT-BUTYL-N-(6-(2-HYDROXYETHOXY)-5-(2-METHOXYPHENOXY)-2,2''-BIPYRIMIDIN-4-YL)BENZENESULFONAMIDE
  • 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]benzenesulfonamide
  • 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide
  • n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]-4-tert-butyl-benzenesulfonamide
  • 4-(1,1-DiMethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-Methoxyphenoxy)[2,2'-bipyriMidin]-4-yl]benzenesulfonaMide
  • Actelion
  • 147536-97-8
  • 147536-98-8
  • C27H29N5O6S
  • Stable Isotopes
  • -
  • Bases & Related Reagents
  • Intermediates & Fine Chemicals
  • Nucleotides
  • Pharmaceuticals
  • Aromatics
  • Heterocycles
  • Sulfur & Selenium Compounds
  • API
  • Free Base API
  • Inhibitors
Copyright 2019 © ChemicalBook. All rights reserved