SML2020
阿曲生坦 盐酸盐
≥98% (HPLC), ETA receptor antagonist, powder
别名:
2R-（4-甲氧基苯基）-4S-（1,3-苯并二恶唑-5-基）-1-（N，N-二（正丁基）氨基羰基甲基）-吡咯烷-3R-羧酸盐酸盐, ABT-627盐酸盐, 盐酸A-147627, （2R，3R，4S）-4-（1,3-苯并二恶唑-5-基）-1- [2-（二丁基氨基）-2-氧乙基] -2-（4-甲氧基苯基）-3-吡咯烷羧酸盐酸盐
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选择尺寸
关于此项目
经验公式（希尔记法）:
C29H38N2O6 · HCl
化学文摘社编号:
分子量:
547.08
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
产品名称
阿曲生坦 盐酸盐, ≥98% (HPLC)
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
SMILES string
[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 key
IJFUJIFSUKPWCZ-SQMFDTLJSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
相关类别
Biochem/physiol Actions
选择性内皮素 ETA 受体拮抗剂
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。
General description
阿曲生坦也已用于治疗心血管疾病。
存储类别
11 - Combustible Solids
wgk
WGK 3
Margien G S Boels et al.
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
Carmen De Miguel et al.
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
Determination of atrasentan by high performance liquid chromatography with fluorescence detection in human plasma.
Bryan P D, et al.
Biomedical Chromatography, 15(8), 525-533 (2001)
Chunhua Jin et al.
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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