阿曲生坦 - CAS:173937-91-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	阿曲生坦
英文名称:	Atrasentan
别名:	阿曲生坦 ABT-627; (+)-A 127722; A-147627
CAS No:	173937-91-2	分子式:	C₂₉H₃₈N₂O₆	分子量:	542.69
CAS No:	173937-91-2
分子式:	C₂₉H₃₈N₂O₆
分子量:	542.69

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A11465 阿曲生坦 (psaitong)

相关产品

包装规格：

10mg in glass bottle

产品描述：

基本信息

产品编号：	A11465
产品名称：	Atrasentan
CAS:	173937-91-2	储存条件	粉末	-20℃	四年
分子式：	C29H38N2O6		溶于液体	-80℃	二年
分子量：	542.69
化学名：	(2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

生物活性

产品描述	一种有效的内皮素受体(endothelin receptor)拮抗剂，抑制ETA的活性，IC50值为0.0551nM。
靶点	IC50:0.055nM (ETA)
体外研究	Atrasentan (ABT-627,0-50μM) 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 50μM).It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11μM).
体内研究	Atrasentan (3mg/kg,p.o.) inhibits the pressor response induced by big endothelin-1 (1nmol/kg) in pithed rats.Aatrasentan (ABT-627,10mg/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.

推荐实验方法(仅供参考)

激酶实验：

Cells are incubated and treated with Atrasentan.They are then washed twice with PBS and lysed in ice-cold lysis buffer [20mM Tris (pH 7.4),150mM NaCl,1% Triton X-100,1mM EDTA,1mM EGTA,2.5mM sodium PPi,1mM β-glycerophosphate,1mM sodium orthovanadate,1μg/mL leupeptin,and 1mM PMSF].The extracts are centrifuged to remove cellular debris,and the protein content of the supernatants is determined using the bicinchoninic acid (BCA) protein assay reagent. Proteins (150μg) are incubated with gentle rocking at 4℃ overnight with immobilized Akt antibody cross-linked to agarose hydrazide beads.After the Akt is selectively immunoprecipitated from the cell lysates,the immunoprecipitated products are washed twice with lysis buffer and twice with kinase assay buffer [25mM Tris (pH 7.5),10mM MgCl2,5mM β-glycerol phosphate,0.1mM sodium orthovanadate,2mM DTT] and then resuspended in 40μL of kinase assay buffer containing 200μM ATP and 1μg GSK-3α/β fusion protein.The kinase assay reaction is allowed to proceed at 30℃ for 30 min and stopped by the addition of Lamelli SDS sample buffer.Reaction products are resolved by 10% SDS-PAGE,followed by Western blotting with antiphosphorylated GSK-3α/β antibody.For analysis of the total amount of Akt,40μg of protein from the lysate samples are resolved by 10% SDS-PAGE,followed by Western blotting with anti-Akt antibody.

细胞实验:

All three prostate cancer cell lines (LNCaP,C4-2b,and PC-3 cells) are seeded at a density of 3×103 cells per well in 96-well microtiter culture plates.After overnight incubation,the medium is removed and replaced with a fresh medium containing different concentrations of ABT-627 (0-5μM) diluted from a 10-mM stock. After 72h of incubation with drug,20μL of MTT solution (5mg/mL in PBS) are added to each well and incubated further for 2h.Upon termination,the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in isopropanol (100μL).The plates are mixed for 30 min on a gyratory shaker,and the absorbance is measured at 595nm on a plate reader.

动物实验:

YM598 (0.3,1,and 3mg/kg),atrasentan (0.3,1,and 3mg/kg),or 0.5% methyl cellulose as vehicle is orally administered to rats with a dosing cannula.Dosing volume of the test substances and vehicle is set at 5mL/kg.Approximately 20 min after administration of compounds,the rats are anesthetized with sodium pentobarbital,and then pithed and ventilated 30 min after dosing.Approximately 1h after oral administration of compounds,big endothelin-1 (1nmol/kg) is intravenously administered,and blood pressure is measured.In these two experiments,the dose of test compound that cause 50% inhibition (ID50) of the big endothelin-1-induced increase in diastolic blood pressure is determined by linear regression analysis.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果