| Identification | Back 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 Properties | Back 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 Information | Back 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) |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|