CAS NO: | 195733-43-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Atrasentan hydrochloride (ABT-627 hydrochloride) is a selectiveendothelin A receptorantagonist with anIC50of 0.0551 nM forETA[1]. | ||||||||||||||||
IC50& Target | IC50: 0.055 nM (ETA) | ||||||||||||||||
体外研究 (In Vitro) | Atrasentan hydrochloride (ABT-627 hydrochloride) (0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth[2]. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50in MDCKII-BCRP cells=59.8±11 μM)[3]. | ||||||||||||||||
体内研究 (In Vivo) | Atrasentan hydrochloride (ABT-627 hydrochloride) (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats[1]. Aatrasentan (ABT-627, 10 mg/kg, i.p.) inhibits the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 547.08 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C29H39ClN2O6 | ||||||||||||||||
CAS 号 | 195733-43-8 | ||||||||||||||||
中文名称 | 盐酸阿曲生坦 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 28.57 mg/mL(52.22 mM;Need ultrasonic) H2O : 0.5 mg/mL(0.91 mM;ultrasonic and warming and adjust pH to 4 with HCl and heat to 60℃) 0.1 M HCL :< 1 mg/mL (ultrasonic;warming;adjust pH to 1 with HCl;heat to 60℃)(insoluble) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|