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CAS No.: 195733-43-8

Atrasentan HCl/盐酸阿曲生坦 Catalog No. CSN13753

Synonyms: ABT-627 hydrochloride;(+)-A 127722 hydrochloride;A-147627 hydrochloride

Atrasentan HCl is an endothelin receptor antagonist (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.

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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

描述Endothelin is a potent vasoconstrictive 21-amino acid peptide implicated in the pathogenesis of various cardiovascular diseases. Endothelin ET_A receptors can mediate contractive and mitogenic actions of endothelin. Atrasentan HCl is a selective endothelin ET_A receptor antagonist with K_i values of 0.0551±0.0267nM and 4.80±0.314nM in human coronary artery smooth muscle cells and human melanoma SK-Mel-28 cells, respectively. The calculated selectivity ratio of atrasentan HCl for endothelin ET_A versus ET_B receptors is 87. Intravenous or oral administration of atrasentan HCl significantly and dose-dependently suppressed big endothelin-1-induced pressor responses in pithed rats with ID_50M values of 0.020mg/kg and 0.787mg/kg, respectively^[3].
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
NCT00134056	Metastatic Cancer ... more >> Prostate Cancer Collapse <<	Phase 3	Completed	-	-
NCT00653328	Fallopian Tube Cancer ... more >> Ovarian Cancer Peritoneal Cavity Cancer Collapse <<	Phase 2	Terminated(Abbott (drug manufa... more >>cturer) discontinued manufacture of ABT-627) Collapse <<	-	United States, Georgia ... more >> Central Georgia Hematology Oncology Associates, P.C. Macon, Georgia, United States, 31201 United States, Kentucky Kentuckiana Cancer Institute Louisville, Kentucky, United States, 40202 United States, Tennessee The Jones Clinic Germantown, Tennessee, United States, 38138 Jackson-Madison County Hospital Jackson, Tennessee, United States, 383013956 St. Thomas Health Services Nashville, Tennessee, United States, 37205 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 Collapse <<
NCT00134056	-	-	Completed	-	-

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参考文献

[1] Banerjee S, Hussain M, et al. In vitro and in vivo molecular evidence for better therapeutic efficacy of ABT-627 and taxotere combination in prostate cancer. Cancer Res. 2007 Apr 15;67(8):3818-26.
[2] Yuyama H, Noguchi Y, et al. Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist. Eur J Pharmacol. 2004 Sep 13;498(1-3):171-7.
[3] Yuyama H, Noguchi Y, Fujimori A, et al. Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist. Eur J Pharmacol. 2004;498(1-3):171-177.

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
- 1.8279 mL
- 9.1394 mL
- 18.2788 mL
- 5 mM
- 0.3656 mL
- 1.8279 mL
- 3.6558 mL
- 10 mM
- 0.1828 mL
- 0.9139 mL
- 1.8279 mL

技术信息

CAS号

195733-43-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H39ClN2O6

运输

蓝冰

分子量

547.08

别名

ABT-627 hydrochloride;(+)-A 127722 hydrochloride;A-147627 hydrochloride;ABT-627;Abbott-147627;Atrasentan HCl;(+)A 127722;A 127722;NSC720763;A147627;US brand name: Xinlay;盐酸阿曲生坦

溶解度

DMSO	95.0 mg/mL (173.6 mM) warming
Water	12.0 mg/mL (21.9 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

NCT00134056	Metastatic Cancer ... more >> Prostate Cancer Collapse <<	Phase 3	Completed	-	-
NCT00653328	Fallopian Tube Cancer ... more >> Ovarian Cancer Peritoneal Cavity Cancer Collapse <<	Phase 2	Terminated(Abbott (drug manufa... more >>cturer) discontinued manufacture of ABT-627) Collapse <<	-	United States, Georgia ... more >> Central Georgia Hematology Oncology Associates, P.C. Macon, Georgia, United States, 31201 United States, Kentucky Kentuckiana Cancer Institute Louisville, Kentucky, United States, 40202 United States, Tennessee The Jones Clinic Germantown, Tennessee, United States, 38138 Jackson-Madison County Hospital Jackson, Tennessee, United States, 383013956 St. Thomas Health Services Nashville, Tennessee, United States, 37205 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 Collapse <<
NCT00134056	-	-	Completed	-	-
NCT00653328	-	-	Terminated(Abbott (drug manufa... more >>cturer) discontinued manufacture of ABT-627) Collapse <<	-	-
NCT00017264	Brain and Central Nervous Syst... more >>em Tumors Collapse <<	Phase 1	Completed	-	United States, Alabama ... more >> University of Alabama at Birmingham Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3300 United States, Florida H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612-9497 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231-2410 United States, Massachusetts Massachusetts General Hospital Cancer Center Boston, Massachusetts, United States, 02114 United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Comprehensive Cancer Center at Wake Forest University Winston-Salem, North Carolina, United States, 27157-1082 United States, Ohio Cleveland Clinic Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania Abramson Cancer Center at University of Pennsylvania Medical Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas University of Texas Health Science Center at San Antonio San Antonio, Texas, United States, 78284-7811 Collapse <<
NCT00046943	Prostate Cancer	Phase 3	Completed	-	United States, California ... more >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095-1738 Collapse <<
NCT00039429	Kidney Cancer	Phase 2	Completed	-	-

Atrasentan HCl/盐酸阿曲生坦 Catalog No. CSN13753

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