西他生坦

• 常用名: 西他生坦
• 英文名: sitaxsentan
• CAS号: 184036-34-8
• 分子量: 454.90500
• 密度: 1.6g/cm3
• 沸点: 600.4ºC at 760 mmHg
• 分子式: C₁₈H₁₅ClN₂O₆S₂
• 熔点: N/A
• 闪点: 316.9ºC

西他生坦用途

Sitaxsentan (IPI 1040; TBC 11251)是选择性内皮素A(ETA)受体拮抗剂。

西他生坦名称

• 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

西他生坦生物活性

• 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.

西他生坦物理化学性质

• 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
• InChIKey: PHWXUGHIIBDVKD-UHFFFAOYSA-N
• SMILES: Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2
• 蒸汽压: 2.25E-14mmHg at 25°C
• 折射率: 1.687
• 储存条件: 2-8℃

西他生坦靶点实验

查看更多实验

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression 来源：NCGC External Id：SNCA-p-activity-luciferase

实验名称：Cytochrome P450 Family 1 Subfamily A Member 2 (CYP1A2) small molecule antagonists: lu... 来源：824 External Id：CYP273

实验名称：Relative affinity for human ETA over ETB receptors. 来源：ChEMBL 靶标：Endothelin receptor type B External Id：CHEMBL841076

实验名称：p53 small molecule agonists, cell-based qHTS assay: qHTS cell viability counter scree... 来源：824 靶标：N/A External Id：P53600

实验名称：p53 small molecule agonists, cell-based qHTS assay with rat liver microsomes: qHTS ce... 来源：824 靶标：N/A External Id：P53MS958

实验名称：p53 small molecule agonists, cell-based qHTS assay with rat liver microsomes: Summary 来源：824 External Id：P53MS482

实验名称：p53 small molecule agonists, cell-based qHTS assay 来源：824 External Id：P53344

实验名称：p53 small molecule agonists, cell-based qHTS assay with human liver microsomes 来源：824 靶标：tumor suppressor p53 [Homo sapiens] External Id：P53MS233

实验名称：p53 small molecule agonists, cell-based qHTS assay with human liver microsomes: qHTS ... 来源：824 靶标：N/A External Id：P53MS837

实验名称：p53 small molecule agonists, cell-based qHTS assay with rat liver microsomes 来源：824 靶标：tumor suppressor p53 [Homo sapiens] External Id：P53MS898

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西他生坦英文别名

• Sitaxsentan
• Sitax