Title: Clazosentan
CAS Registry Number: 180384-56-9
CAS Name: N-[6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(1H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-methyl-2-pyridinesulfonamide
Additional Names: 5-methylpyridine-2-sulfonic acid 6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-1H-tetrazol-5-ylpyridin-4-yl)pyrimidin-4-ylamide
Molecular Formula: C25H23N9O6S
Molecular Weight: 577.57
Percent Composition: C 51.99%, H 4.01%, N 21.83%, O 16.62%, S 5.55%
Literature References: Nonpeptide selective endothelin ETA receptor antagonist. Prepn: V. Breu et al., WO 9619459; eidem, US 6004965 (1996, 1999 both to Hoffmann-La Roche). Pharmacology and receptor binding study: S. Roux et al., J. Pharmacol. Exp. Ther. 283, 1110 (1997). Clinical pharmacology: T. J. L. Vuurmans et al., Hypertension 41, 1253 (2003). Cerebrovascular characterization: H. Vatter et al., J. Neurosurg. 102, 1101, 1108 (2005). Clinical effect on vasospasm following subarachnoid hemorrhage: P. Vajkoczy et al., ibid. 103, 9 (2005). Review of development and therapeutic potential: D. Uhlmann, Curr. Opin. Invest. Drugs 7, 272-281 (2006).
Properties: White substance from acetonitrile, mp 239-241°.
Melting point: mp 239-241°
Derivative Type: Disodium salt
CAS Registry Number: 503271-02-1
Manufacturers' Codes: AXV-034343; Ro-61-1790; VML-588
Molecular Formula: C25H21N9Na2O6S
Molecular Weight: 621.54
Percent Composition: C 48.31%, H 3.41%, N 20.28%, Na 7.40%, O 15.44%, S 5.16%
Properties: pKa1 4.5; pKa2 3.3. Soly in water: 25% at physiol pH.
pKa: pKa1 4.5; pKa2 3.3
Therap-Cat: In treatment of cerebral vasospasm.
Keywords: Vasoprotectant; Endothelin Receptor Antagonist. |