Tezosentan
Title: Tezosentan
CAS Registry Number: 180384-57-0
CAS Name: N-[6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(1H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-(1-methylethyl)-2-pyridinesulfonamide
Additional Names: 5-isopropylpyridine-2-sulfonic acid 6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-1H-tetrazol-5-ylpyridin-4-yl)pyrimidin-4-ylamide
Molecular Formula: C27H27N9O6S
Molecular Weight: 605.62
Percent Composition: C 53.55%, H 4.49%, N 20.82%, O 15.85%, S 5.29%
Literature References: Dual endothelin (ETA/ETB) receptor antagonist. Prepn: V. Breu et al., WO 9619459; eidem, US 6004965 (1996, 1999 both to Hoffmann-La Roche). Pharmacology and receptor binding: M. Clozel et al., J. Pharmacol. Exp. Ther. 290, 840 (1999). Clinical pharmacokinetics: J. Dingemanse et al., Br. J. Clin. Pharmacol. 53, 355 (2002). Clinical evaluation in advanced heart failure: C. Schalcher et al., Am. Heart J. 142, 340 (2001). LC-MS determn in plasma: P. L. M. van Giersbergen et al., J. Chromatogr. B 792, 369 (2003).
Properties: White solid from acetonitrile, mp 198-200°.
Melting point: mp 198-200°
 
Derivative Type: Sodium salt
CAS Registry Number: 180384-58-1
Manufacturers' Codes: Ro-61-0612
Trademarks: Veletri (Actelion)
Molecular Formula: C27H25N9Na2O6S
Molecular Weight: 649.59
Percent Composition: C 49.92%, H 3.88%, N 19.41%, Na 7.08%, O 14.78%, S 4.94%
Properties: White powder from sodium methylate. pKa1 4.4; pKa2 4.1. Sol in water.
pKa: pKa1 4.4; pKa2 4.1
 
Therap-Cat: In treatment of congestive heart failure.
Keywords: Endothelin Receptor Antagonist.

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