173937-91-2
173937-91-2 结构式
基本信息
(2R,3R,4S)-4-(1,3-苯并二氧戊环-5-基)-1-[2-(二丁基氨基)-2-氧代乙基]-2-(4-甲氧基苯基)吡咯烷-3-羧酸
atrasentan
(+)-A 127722
Atrasentan (ABT-627)
A127722, CID 5310990
(+)-A 127722
ABT-627
A 127722
ABT 627
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
(2S,3S,4R)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-(DIBUTYLAMINO)-2-OXOETHYL]-2-(4-METHOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid
3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-, (2R,3R,4S)-
物理化学性质
常见问题列表
IC50: 0.055 nM (ET A )
Atrasentan (ABT-627, 0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity. 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 (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).
Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model.