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Atrasentan HCl

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Chemical Structure| 195733-43-8 同义名 : ABT-627 hydrochloride;A-147627 hydrochloride;(+)-A 127722 hydrochloride;Atrasentan hydrochloride
CAS号 : 195733-43-8
货号 : A679665
分子式 : C29H39ClN2O6
纯度 : 99%+
分子量 : 547.083
MDL号 : MFCD13194884
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(54.84 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Endothelin is a potent vasoconstrictive 21-amino acid peptide implicated in the pathogenesis of various cardiovascular diseases. Endothelin ETA receptors can mediate contractive and mitogenic actions of endothelin. Atrasentan HCl is a selective endothelin ETA receptor antagonist with Ki 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 ETA versus ETB 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 ID50M values of 0.020mg/kg and 0.787mg/kg, respectively[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.14mL

1.83mL

0.91mL

18.28mL

3.66mL

1.83mL
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.