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180384-57-0

180384-57-0 Structure

180384-57-0 Structure
IdentificationBack Directory
[Name]

TEZOSENTAN
[CAS]

180384-57-0
[Synonyms]

TEZOSENTAN
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
N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide
N-[6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyriMidinyl]-5-(1-Methylethyl)-2-pyridinesulfonaMide
[Molecular Formula]

C27H27N9O6S
[MDL Number]

MFCD00949625
[MOL File]

180384-57-0.mol
[Molecular Weight]

605.62
Chemical PropertiesBack Directory
[Melting point ]

198-200°
[Boiling point ]

761.2±70.0 °C(Predicted)
[density ]

1.432±0.06 g/cm3(Predicted)
[storage temp. ]

Sealed in dry,2-8°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[pka]

2.93±0.10(Predicted)
[color ]

Off-white to gray
Hazard InformationBack Directory
[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)
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