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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
[H]Cl.CCCCN(CCCC)C(CN1C[C@H](C2=CC=C(OCO3)C3=C2)[C@@H](C(O)=O)[C@@H]1C4=CC=C(OC)C=C4)=O
InChI
1S/C29H38N2O6.ClH/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20;/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34);1H/t23-,27-,28+;/m1./s1
InChI 密鑰
IJFUJIFSUKPWCZ-SQMFDTLJSA-N
一般說明
阿曲生坦也已用于治疗心血管疾病。
生化/生理作用
阿曲生坦是一种选择性内皮素 ETA 受体拮抗剂,ETA 的 IC50 为 0.2 nM,而 ETB 受体的 IC50 为 190 nM。它阻断内皮素诱导的细胞增殖,已被研究作为前列腺癌的一种潜在疗法,最近又被用于糖尿病肾病的疗法。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
Determination of atrasentan by high performance liquid chromatography with fluorescence detection in human plasma.
Biomedical Chromatography, 15(8), 525-533 (2001)
Diabetes, 65(8), 2429-2439 (2016-05-22)
Atrasentan, a selective endothelin A receptor antagonist, has been shown to reduce albuminuria in type 2 diabetes. We previously showed that the structural integrity of a glomerular endothelial glycocalyx is required to prevent albuminuria. Therefore we tested the potential of
Scientific reports, 7, 43152-43152 (2017-02-24)
Endothelin-1 (ET-1) promotes renal damage during cardiovascular disease; yet, the molecular mechanisms involved remain unknown. Endoplasmic reticulum (ER) stress, triggered by unfolded protein accumulation in the ER, contributes to apoptosis and organ injury. These studies aimed to determine whether the
The Journal of pharmacology and experimental therapeutics, 351(2), 467-473 (2014-09-06)
Experiments determined whether the combination of endothelin A (ETA) receptor antagonist [ABT-627, atrasentan; (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid] and a thiazide diuretic (chlorthalidone) would be more effective at lowering blood pressure and reducing renal injury in a rodent model of metabolic syndrome compared
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