卡麦角林 - CAS:81409-90-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	卡麦角林促销
英文名称:	Cabergoline
别名:	卡麦角林 FCE-21336
CAS No:	81409-90-7	分子式:	C₂₆H₃₇N₅O₂	分子量:	451.6
CAS No:	81409-90-7
分子式:	C₂₆H₃₇N₅O₂
分子量:	451.6

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C10878 卡麦角林 ≥98% (psaitong)

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包装规格：

5mg 10mg 25mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO（≥ 33 mg/mL）

产品描述：

基本信息

产品编号：	C10878
产品名称：	Cabergoline
CAS:	81409-90-7	储存条件	粉末	-20℃	四年

分子式：	C26H37N5O2		溶于液体	-80℃	6个月
分子量：	451.60			-20℃	1个月
化学名：	1-((6-Allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea
Solubility (25°C)：
体外:	DMSO	90mg/mL (199.29mM)
	Ethanol	90mg/mL (199.29mM)
	Water	Insoluble
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	2.2143mL	11.0717mL	22.1435mL
5mM	0.4429mL	2.2143mL	4.4287mL
10mM	0.2214mL	1.1072mL	2.2143mL
50mM	0.0443mL	0.2214mL	0.4429mL

生物活性

产品描述	一种麦角衍生的多巴胺D2亚类受体激动剂，高亲和力作用于D2，D3和5-HT2B受体，Ki分别为0.7，1.5和1.2。
靶点	Ki:0.7(Dopamine D2 receptor),1.5(Dopamine D3 receptor),1.2(5-HT2B receptor)
体外研究	Cabergoline acts as a potent agonist of D2,D3 and 5-HT2B receptors.Pretreatment with Cabergoline inhibits H2O2-induced neuronal cell death in a dose-dependent manner.In the following experiments,10µM of Cabergoline is used to investigate its neuroprotective effects.MAP2 staining reveals that Cabergoline significantly suppresses the loss of neurons caused by H2 O2 incubation.The detection of apoptotic nuclear condensation suggested that Cabergoline prevents apoptotic cell death following H2O2 exposure.
体内研究	Cabergoline has a longer elimination half-life (63 to 109h) compared with other D2-like receptor agonists,both a longlasting clinical effect following single-dose administration,and an improvement in the quality of life of patients with chronic diseases are expected.The most significant reduction in rapid eye movement (REM) sleep bout number occurred during the light phase,in which Cabergoline-injected female handled mice has 67.3% less REM sleep bouts (F(1,11)=12.892,P=0.004) than Cabergoline-injected females that are restrained,although the greatest number in reduction of REM sleep bouts occurr during the dark phase (82.3% fewer REM sleep bouts;F(1,11)=3.667, P=0.082).In male mice,Cabergoline reduces baseline Prolactin (PRL) levels (98.5%;F(1,6)=13.192,P=0.011) from 5.8±1.3 to 0.08ng/mL within 2 hours of injection.After a 7-day recovery period, PRL levels return to values that are not different from baseline (5.0±0.60ng/mL;F(1,6)=0.715,P=0.43).

推荐实验方法(仅供参考)

细胞实验:

Primary cortical neurons are prepared.Cabergoline (10µM;except for experiments of dose dependency) is applied to cortical cells at DIV 6-7.After 24-hour Cabergoline treatment (except for examination of pretreatment time-dependency of Cabergoline),H2O2 (50µM;except for the dose-dependency of H2O2) is added.All inhibitors and antagonists,including spiperone,U0126,SB203580,SP600125,AP5,and nifedipine are applied 20 min before Cabergoline or H2O2 addition.Lglutamate is added at DIV 7-8 for cell death induction.Cell survival rate is measured by MTT assay.After the indicated treatment with drugs is completed,culture medium is replaced with 200µL fresh medium containing 40µl MTT solution (2.5mg/mL,diluted in PBS) and cells are incubated at 37℃ for 1.5-2.5 hours.Then,200µL lysis buffer containing isopropyl alcohol is applied to each well and mixed by pipetting.Each sample is moved to a 96-well plate and its absorbance at 570nm is measured using an iMark Micro plate leader.Cell survival rate is quantitated by absorbance measurement,because MTT (yellow) is deoxidized to formazan (violet) in proportion to mitochondrial activity.

动物实验:

Mice

Female and male C57BL/6J mice are used.Cabergoline is dissolved in 100% pharmasolve and then diluted with 20% βcyclodextrin in water to yield a final concentration of 0.15-0.5mg/mL Cabergoline.Mice received a 0.3-mg/kg ip injection of Cabergoline or vehicle.All drugs are prepared within 48 hours of experiment and stored at 4℃.Solutions are allowed to reach at room temperature before injection.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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