Sitaxsentan (IPI 1040; TBC-11251) 是选择性内皮素A (ETA) 受体拮抗剂。
| Cas No. | 184036-34-8 |
| 别名 | 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,IPI 1040; TBC-11251 |
| Canonical SMILES | O=S(C1=C(C(CC2=CC3=C(C=C2C)OCO3)=O)SC=C1)(NC4=C(C(C)=NO4)Cl)=O |
| 分子式 | C18H15ClN2O6S2 |
| 分子量 | 454.9 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.IC50 value:Target: ETA receptor [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. |
