Basic information Safety Supplier Related

TEZOSENTAN

Basic information Safety Supplier Related

TEZOSENTAN Basic information

Product Name:
TEZOSENTAN
Synonyms:
  • TEZOSENTAN
  • N-[6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyriMidinyl]-5-(1-Methylethyl)-2-pyridinesulfonaMide
  • N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5
  • N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl
  • N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide
  • RO 610612
  • 2-Pyridinesulfonamide, N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-(1-methylethyl)-
CAS:
180384-57-0
MF:
C27H27N9O6S
MW:
605.62
Product Categories:
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Sulfur & Selenium Compounds
Mol File:
180384-57-0.mol
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TEZOSENTAN Chemical Properties

Melting point:
198-200°
Boiling point:
761.2±70.0 °C(Predicted)
Density 
1.432±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
Soluble in DMSO
pka
2.93±0.10(Predicted)
form 
Solid
color 
Off-white to gray
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TEZOSENTAN Usage And Synthesis

Uses

A potent dual endothelian (ETA/ETB) receptor antagonist optimized from Bosentan (B675900). It is used in the treatment of congestive heart failure.

Uses

A potent dual endothelian (ETA/ETB) receptor antagonist optimized from Bosentan (B675900). Tezosentan is used in the treatment of congestive heart failure.

in vivo

In pithed Wistar rats, Tezosentan dose-dependently inhibits the pressor effect of big ET-1 (P<0.001 at all doses). At the lowest dose tested of 1 mg/kg, Tezosentan inhibits the pressor effect of the various doses of big ET-1 by 50 to 80%. Tezosentan has no effect by itself on blood pressure in these pithed rats. Tezosentan is very effective in a rat model of acute renal failure. ET antagonists have been shown to prevent the vasoconstriction and the renal failure that follow acute renal ischemia in rats[1].

IC 50

ETA: 9.5 (pA2); ETB: 7.7 (pA2)

TEZOSENTANSupplier

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