盐酸阿曲生坦 - CAS:195733-43-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	盐酸阿曲生坦
英文名称:	Atrasentan hydrochloride
别名:	盐酸阿曲生坦;(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-羧酸盐酸盐;((1R,4R)-4-氨基环己基)甲醇 ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride
CAS No:	195733-43-8	分子式:	C₂₉H₃₉ClN₂O₆	分子量:	547.08
CAS No:	195733-43-8
分子式:	C₂₉H₃₉ClN₂O₆
分子量:	547.08

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

A11459 盐酸阿曲生坦 ≥98% (psaitong)

相关产品

包装规格：

5mg in glass bottle

溶解性：

溶于水（12.5mg/mL 超声），溶于DMSO（≥100 mg/mL )

产品描述：

基本信息

产品编号：	A11459
产品名称：	Atrasentan hydrochloride
CAS:	195733-43-8	储存条件	粉末	-20℃	四年

分子式：	C29H39ClN2O6		溶于液体	-80℃	6个月
分子量：	547.08			-20℃	1个月
化学名：	3-Pyrrolidinecarboxylicacid,4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-,hydrochloride (1:1), (2R,3R,4S)-
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.8279 mL	9.1394 mL	18.2789 mL
5mM	0.3656 mL	1.8279 mL	3.6558 mL
10mM	0.1828 mL	0.9139 mL	1.8279 mL

生物活性

产品描述	一种有效的选择性内皮素 A 受体 (endothelin A receptor) 拮抗剂，抑制 ETA 的活性，IC50 值为 0.0551 nM。
靶点	IC50: 0.055 nM (ETA)
体外研究	Atrasentan hydrochloride (ABT-627 hydrochloride) (0-50μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growt.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 hydrochloride (ABT-627 hydrochloride) (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.) inhibits 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)

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 (0-50μM) 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 NSC 10816, 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