| 中文名称： | 卡麦角林 | 中文别名： | 卡麦角林 |
|---|---|---|---|
| 英文名称： | Cabergoline | CAS： | 81409-90-7 |
| 产品分类： | 小分子化合物 | 纯度： | ≥98% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| IC3990 | 索莱宝 | ≥98% | 5mg | 有现货 | 800.00 元 |
| IC3990 | 索莱宝 | ≥98% | 10mg | 有现货 | 1,236.00 元 |
| IC3990 | 索莱宝 | ≥98% | 10mM*1mL in DMSO | 有现货 | 1,540.00 元 |
| IC3990 | 索莱宝 | ≥98% | 1mg | 有现货 | 346.00 元 |
| 标准名称: | 卡麦角林 | 英文名称： | Cabergoline |
|---|---|---|---|
| CAS： | 81409-90-7 | 分子式： | C26H37N5O2 |
| 分子量： | 451.604285955429 | 颜色与性状： | 白色结晶固体 |
| 密度： | 1.2±0.1 g/cm3 | 沸点： | Not available |
| 熔点： | 102-104°C | 水溶性： |
| CAS | 81409-90-7 |
| 中文名称 | 卡麦角林 |
| 英文名称 | Cabergoline |
| 别名 | FCE-21336 |
| 分子式 | C26H37N5O2 |
| 分子量 | 451.6 |
| 规格 | 10mg ; 10mM*1mL in DMSO ; 5mg ; 1mg |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 级别 | Cell Culture |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | EINECS 200-419-0 |
| MDL | MFCD00867887 |
| SMILES | C=CCN1[C@](C2C[C@@H](C(N(CCCN(C)C)C(NCC)=O)=O)C1)([H])CC3=CNC4=CC=CC2=C43 |
| InChIKey | KORNTPPJEAJQIU-KJXAQDMKSA-N |
| InChI | InChI=1S/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21-,23-/m1/s1 |
| PubChem CID | 54746 |
| 靶点 | Dopamine Receptor |
| 通路 | Neuronal Signaling;GPCR & G Protein |
| 背景说明 | 是一种长效多巴胺(dopamine)激动剂和催乳激素(prolactin)抑制剂。 |
| 生物活性 | Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).[1-2] |
| IC50 | Ki: 0.7(Dopamine D2 receptor)，1.5(Dopamine D3 receptor)，1.2(5-HT2B receptor)[1] |
| In Vitro | 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，10 μM of Cabergoline is used to investigate its neuroprotective effects. MAP2 staining reveals that Cabergoline significantly suppresses the loss of neurons caused by H2O2 incubation. The detection of apoptotic nuclear condensation suggested that Cabergoline prevents apoptotic cell death following H2O2 exposure[1]. |
| In Vivo | Cabergoline has a longer elimination half-life(63 to 109 h)compared with other D2-like receptor agonists，both a long-lasting clinical effect following single-dose administration，and an improvement in the quality of life of patients with chronic diseases are expected[1]. 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 0.08 ng/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±0.60 ng/mL; F(1，6)=0.715，P=0.43)[2]. |
| 细胞实验 | Primary cortical neurons are prepared. Cabergoline(10 μM; 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(50 μM; 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. L-glutamate 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 200 μL fresh medium containing 40 μl MTT solution(2.5 mg/mL，diluted in PBS)and cells are incubated at 37°C for 1.5-2.5 hours. Then，200 μL 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 570 nm 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[1]. |
| 动物实验 | Mice[2]Female and male C57BL/6J mice are used.Cabergoline is dissolved in 100% pharmasolve and then diluted with 20% β-cyclodextrin in water to yield a final concentration of 0.15-0.5 mg/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°C. Solutions are allowed to reach at room temperature before injection. |
| 数据来源文献 | [1]. Odaka H， et al. Cabergoline， dopamine D2 receptor agonist， prevents neuronal cell death under oxidative stress via reducing excitotoxicity. PLoS One. 2014 Jun 10;9(6):e99271. [2]. Jefferson F， et al. A dopamine receptor d2-type agonist attenuates the ability of stress to alter sleep in mice. Endocrinology. 2014 Nov;155(11):4411-21 |
| 单位 | 瓶 |
| 1mM-5mg | 11.0717mL |
| 1mM-1mg | 2.2143mL |
| 1mM-10mg | 22.1435mL |
| 5mM-1mg | 0.4429mL |
| 5mM-5mg | 2.2143mL |
| 5mM-10mg | 4.4287mL |
| 10mM-1mg | 0.2214mL |
| 10mM-5mg | 1.1072mL |
| 10mM-10mg | 2.2143mL |
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| 企业认证： | 已认证 | 企业性质： | 生产研发 |
|---|---|---|---|
| 主营产品： | 透明质酸酶，牛睾丸 ； 盐酸环丙沙星无菌溶液(20mg/ml) ； L-苹果酸(10mM in DMSO) ； Z-VAD(OMe)-FMK(10mM in DMSO，无菌） ； 埃文斯蓝(10mM in DMSO，无菌） ； | 供货范围： | 试剂 |
| 产品目录： | 119902 | 品牌： | 索莱宝 |
| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| - | 索莱宝 | 10ml | 北京 |
