| 溶解性 | 25°C: DMSO |
| 存贮条件 | 储存温度-20°C |
| 生化机理 | Description:IC50 Value: 0.0551 nM (for ET A receptor) [1]Atrasentan (A-147627) is an endothelin antagonist receptor being developed at Abbott Laboratories for the treatment of prostate cancer.in vitro: The combination of Atrasentan with Taxotere was more effective in the inhibition of cell viability and induction of apoptosis in LNCaP and C4-2b cells (androgen receptor positive) but not in PC-3 cells[2]. Atrasentan profoundly induced several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It was a moderate P-gp inhibitor (IC(50) in P388/dx cells = 15.1 ± 1.6 μM) and a weak BCRP inhibitor (IC(50) in MDCKII-BCRP cells = 59.8 ± 11 μM). BCRP or P-gp overexpressing cells were slightly more resistant towards antiproliferative effects of atrasentan [5].in vivo: ABT-627 did reduce the accumulation of macrophages in both stains (36 to 53%) whereas it blocked by 76% the influx of eosinophils in Balb/c but not in C57Bl/6 mice [3]. Atrasentan was administered orally via drinking water at 3 mg kg-1 per day over 28 days. All diabetic mice developed similar hyperglycaemia (27-30 mmol l-1). Atrasentan treatment significantly improved left ventricular systolic and diastolic function in response to exogenous norepinephrine, but there were no differences between genotypes [4].Clinical trial: Atrasentan and Zometa for Men With Prostate Cancer Metastatic to Bone . Phase2 |
阿曲生坦
Atrasentan （订货以英文为准）
编号：A125773
CAS号：173937-91-2
分子式：C29H38N2O6
分子量：510.62
| 产品名称 | Atrasentan |
| 中文名称 | 阿曲生坦 |
| CAS号 | 173937-91-2 |
| 分子式（M.F.） | C29H38N2O6 |
| 分子量（M.W.） | 510.62 |
| 储存条件 | -20°C储存 |
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