Structural Formula Vector Image
Title: Sitaxsentan
CAS Registry Number: 184036-34-8
CAS Name: N-(4-Chloro-3-methyl-5-isoxazolyl)-2-[(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide
Additional Names: N-(4-chloro-3-methyl-5-isoxazolyl)-2-[3,4-(methylenedioxy)-6-methyl]phenylacetyl-3-thiophenesulfonamide
Manufacturers' Codes: IPI-1040; TBC-11251
Molecular Formula: C18H15ClN2O6S2
Molecular Weight: 454.90
Percent Composition: C 47.53%, H 3.32%, Cl 7.79%, N 6.16%, O 21.10%, S 14.10%
Literature References: Selective endothelin A (ETA) receptor antagonist. Prepn: M. F. Chan et al., WO 9631492 ; eidem, US 5594021 (1996, 1997 both to Texas Biotech.); C. Wu et al., J. Med. Chem. 40, 1690 (1997). Pharmacology: R. G. Tilton et al., Pulm. Pharmacol. Ther. 13, 87 (2000). Clinical evaluation in heart failure: M. M. Givertz et al., Circulation 101, 2922 (2000); in pulmonary arterial hypertension: D. Langleben et al., Chest 126, 1377 (2004). Review of development and therapeutic potential: E. M. Horn et al., Expert Opin. Invest. Drugs 13, 1483-1492 (2004).
Properties: Yellow powder, mp 42-45°.
Melting point: mp 42-45°
Derivative Type: Sodium salt
CAS Registry Number: 210421-74-2
Trademarks: Thelin (Encysive)
Molecular Formula: C18H14ClNaN2O6S2
Molecular Weight: 476.89
Percent Composition: C 45.33%, H 2.96%, Cl 7.43%, Na 4.82%, N 5.87%, O 20.13%, S 13.45%
Therap-Cat: Antihypertensive. In treatment of chronic heart failure.
Keywords: Antihypertensive; Endothelin Receptor Antagonist.

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