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CAS No.: 210421-74-2

Sitaxsentan sodium Catalog No. CSN12974

Synonyms: IPI 1040 sodium;TBC11251 sodium;TBC11251 Sodium Salt

Sitaxsentan sodium has selectory antagonism of endothelin A (ETA) receptor with the IC50 and Ki value of 1.4 nM and 0.43 nM respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Endothelin Receptor A

IC50:1.4nM
描述G protein-coupled receptor (GPCR) agonists through their receptors can transactivate protein tyrosine kinase receptors such as epidermal growth factor receptor and serine/threonine kinase receptors most notably transforming growth factor (TGF)-β receptor (TβRI). Several GPCR agonists such as Ang II, thrombin, ET-1 can mediate the transactivation of a multitude of protein tyrosine kinase receptors^[3]. Endothelin-1 (ET-1) is a potent vasoconstrictor peptide thought to play a critical role in the pathogenesis and progression of PAH. The biological effects of ET-1 are mediated through the endothelin receptor subtype A (ETA) and endothelin receptor subtype B (ETB). Sitaxsentan Sodium is an ETA-selective endothelin receptor antagonists (ERAs) with IC₅₀ value of 1.4 nM^[4]. Patients with New York Heart Association (NYHA) functional class II-IV PAH treated with 100 mg sitaxsentan showed statistically significant improvements in 6-minute walk distance (6MWD) (35 m placebo corrected improvement, p<0.01) and 29% of the sitaxsentan 100-mg patients improved by at least one functional class without any deteriorations^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00593905	-	-	Unknown	July 2013	United States, Pennsylvania ... more >> Allegheny General Hospital Recruiting Pittsburgh, Pennsylvania, United States, 15212 Contact: Andrea L Nowicki, BA 412-359-3653 anowicki@wpahs.org Contact: Raymond L Benza, MD 412.359.3584 rbenza@wpahs.org Principal Investigator: Raymond L Benza, MD Collapse <<
NCT00810732	Chronic Kidney Disease ... more >> CRD Collapse <<	Phase 2	Completed	-	United Kingdom ... more >> Pfizer Investigational Site Edinburgh, Scotland, United Kingdom, EH4 2XU Collapse <<
NCT00796666	Pulmonary Arterial Hypertensio... more >>n Pulmonary Hypertension Collapse <<	Phase 3	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0969 mL
- 10.4846 mL
- 20.9692 mL
- 5 mM
- 0.4194 mL
- 2.0969 mL
- 4.1938 mL
- 10 mM
- 0.2097 mL
- 1.0485 mL
- 2.0969 mL

技术信息

CAS号

210421-74-2

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H14ClN2NaO6S2

运输

蓝冰

分子量

476.89

别名

IPI 1040 sodium;TBC11251 sodium;TBC11251 Sodium Salt;Sitaxentan (sodium salt);TBC-11251;Sitaxentan sodium

溶解度

DMSO	95.0 mg/mL (199.2 mM) warming

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00593905	-	-	Unknown	July 2013	United States, Pennsylvania ... more >> Allegheny General Hospital Recruiting Pittsburgh, Pennsylvania, United States, 15212 Contact: Andrea L Nowicki, BA 412-359-3653 anowicki@wpahs.org Contact: Raymond L Benza, MD 412.359.3584 rbenza@wpahs.org Principal Investigator: Raymond L Benza, MD Collapse <<
NCT00810732	Chronic Kidney Disease ... more >> CRD Collapse <<	Phase 2	Completed	-	United Kingdom ... more >> Pfizer Investigational Site Edinburgh, Scotland, United Kingdom, EH4 2XU Collapse <<
NCT00796666	Pulmonary Arterial Hypertensio... more >>n Pulmonary Hypertension Collapse <<	Phase 3	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-
NCT00796666	-	-	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-
NCT00795639	Pulmonary Arterial Hypertensio... more >>n Pulmonary Hypertension Collapse <<	Phase 3	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-
NCT00796510	-	-	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury) Collapse <<	-	-
NCT00981968	Healthy	Phase 1	Completed	-	United States, California ... more >> Pfizer Investigational Site Glendale, California, United States, 91206 Collapse <<
NCT00796510	Pulmonary Arterial Hypertensio... more >>n Pulmonary Hypertension Collapse <<	Phase 3	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury) Collapse <<	-	United States, California ... more >> Pfizer Investigational Site Fountain Valley, California, United States, 92708 Romania Pfizer Investigational Site Cluj Napoca, Romania, 400 001 Ukraine Pfizer Investigational Site Kyiv, Ukraine Collapse <<
NCT00744211	-	-	Completed	-	-
NCT00995566	-	-	Terminated(The trial was prema... more >>turely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.") Collapse <<	-	Belgium ... more >> Pfizer Investigational Site Bruxelles, Belgium, 1070 Pfizer Investigational Site Leuven, Belgium, 3000 France Pfizer Investigational Site Nice, France, 06000 Germany Pfizer Investigational Site Hannover, Germany, 30625 Collapse <<
NCT00995566	-	-	Terminated(The trial was prema... more >>turely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.") Collapse <<	-	-
NCT00811018	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 3	Terminated(This trial was prem... more >>aturely terminated on Dec 9 2010 due to safety concerns, specifically emerging evidence of hepatic injury.) Collapse <<	-	-
NCT00795639	-	-	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-
NCT00034307	Pulmonary Hypertension	Phase 2 Phase 3	Unknown	-	-
NCT00811018	-	-	Terminated(This trial was prem... more >>aturely terminated on Dec 9 2010 due to safety concerns, specifically emerging evidence of hepatic injury.) Collapse <<	-	-
NCT01204853	Hypertension, Pulmonary	Phase 3	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	Japan ... more >> Pfizer Investigational Site Nagoya, Aichi, Japan Pfizer Investigational Site Shinjyuku-ku, Tokyo, Japan Collapse <<
NCT01210443	-	-	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-
NCT00744211	Heart Disease	Not Applicable	Completed	-	United States, South Carolina ... more >> Ralph H. Johnson VA Medical Center, Charleston, SC Charleston, South Carolina, United States, 29401-5799 Collapse <<
NCT01204853	-	-	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	-
NCT01445873	-	-	Completed	-	-
NCT01445873	-	-	Completed	-	-
NCT00080457	Pulmonary Hypertension	Phase 3	Completed	-	United States, Texas ... more >> Encysive Pharmaceuticals Houston, Texas, United States, 77401 Collapse <<
NCT01210443	Hypertension, Pulmonary	Phase 3	Terminated(Safety Issue The tr... more >>ial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.) Collapse <<	-	Japan ... more >> Pfizer Investigational Site Nagoya, Aichi, Japan Pfizer Investigational Site Shinjyuku-ku, Tokyo, Japan Collapse <<
NCT00303498	Diastolic Heart Failure	Phase 2	Completed	-	-

Sitaxsentan sodium Catalog No. CSN12974

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