184036-34-8

• 常用中文名：西他生坦
• 常用英文名：sitaxsentan
• CAS号：184036-34-8
• 分子式：C₁₈H₁₅ClN₂O₆S₂
• 分子量：454.90500
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 内皮素受体
• 发布时间：2019-01-09 19:41:50
• 更新时间：2025-08-26 23:12:55
• Sitaxsentan (IPI 1040; TBC 11251)是选择性内皮素A(ETA)受体拮抗剂。

名称

• 中文名: N-(4-氯-3-甲基-5-异恶唑基)-2-[(2-甲基-4,5-亚甲二氧基苯基)乙酰]噻吩-3-磺酰胺
• 英文名: N-(4-Chloro-3-methylisoxazol-5-yl)-2-(2-(6-methylbenzo-[d][1,3]dioxol-5-yl)acetyl)thiophene-3-sulfonamide
• 中文别名: 司他生坦
• 英文别名: Sitaxsentan; Sitax

物化性质

• 密度: 1.6g/cm3
• 沸点: 600.4ºC at 760 mmHg
• 分子式: C₁₈H₁₅ClN₂O₆S₂
• 分子量: 454.90500
• 闪点: 316.9ºC
• 精确质量: 454.00600
• PSA: 144.35000
• LogP: 5.11500
• 蒸汽压: 2.25E-14mmHg at 25°C
• 折射率: 1.687
• 储存条件: 2-8℃

生物活性

• 描述: Sitaxsentan (IPI 1040; TBC 11251)是选择性内皮素A(ETA)受体拮抗剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 内皮素受体
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Chin M, Levy RD, Yoshida EM, Byrne MF.Sitaxsentan-induced acute severe hepatitis treated with glucocorticoid therapy.Can Respir J. 2012 Jan-Feb;19(1):e1-2.

  [2]. Sandoval J, et al. STRIDE-4 investigators.Safety and efficacy of sitaxsentan 50 and 100 mg in patients with pulmonary arterial hypertension.Pulm Pharmacol Ther. 2012 Feb;25(1):33-9. Epub 2011 Nov 2.

  [3]. Safdar Z. Effect of transition from sitaxsentan to ambrisentan in pulmonary arterial hypertension.Vasc Health Risk Manag. 2011;7:119-24. Epub 2011 Mar 2.

  [4]. Rondelet B, et al. Sildenafil added to sitaxsentan in overcirculation-induced pulmonary arterial hypertension.Am J Physiol Heart Circ Physiol. 2010 Oct;299(4):H1118-23. Epub 2010 Aug 6.

  [5]. Kaehler, et al. Successful treatment of portopulmonary hypertension with the selective endothelin receptor antagonist Sitaxentan. Wien Klin Wochenschr. 2011 Apr;123(7-8):248-52. Epub 2011 Mar 31.

合成路线

1008726-80-4 210421-71-9 ~% 184036-34-8

文献：Wu, Chengde; Chan, Ming F.; Stavros, Fiona; Raju; Okun, Ilya; Mong, Seymour; Keller, Karin M.; Brock, Tommy; Kogan, Timothy P.; Dixon, Richard A. F. Journal of Medicinal Chemistry, 1997 , vol. 40, # 11 p. 1690 - 1697

117661-72-0 ~69% 184036-34-8

文献：Texas Biotechnology Corporation Patent: US6432994 B1, 2002 ; US 6432994 B1

117661-72-0 210421-71-9 ~% 184036-34-8

文献：Chen, Jinling; Koppenol, Sandy; Rajewski, Lian; Trammel, Andrew; Amsberry, Kent; Schoeneman, Aaron Patent: US2008/76812 A1, 2008 ; Location in patent: Page/Page column 10 ;

20850-43-5 117661-72-0 210421-71-9 ~% 184036-34-8

文献：ENCYSIVE PHARMACEUTICALS, INC. Patent: WO2007/106494 A2, 2007 ; Location in patent: Page/Page column 39-40 ;

210421-71-9 ~% 184036-34-8

文献：Given, Bruce D.; Dixon, Richard A.F. Patent: US2008/85313 A1, 2008 ; Location in patent: Page/Page column 15 ;

117661-72-0 184040-74-2 ~73% 184036-34-8

文献：Texas Biotechnology Corp. Patent: US6342610 B2, 2002 ; Location in patent: Page column 126 ; US 6342610 B2

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