1、Product Data SheetCabergolineCat. No.: HY-15296CAS No.: 81409-90-7分式: CHNO分量: 451.6作靶點(diǎn): Dopamine Receptor; Autophagy作通路: GPCR/G Protein; Neuronal Signaling; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33 mg/mL (73.07 mM)H2O : 0.1 mg/mL (insoluble)*

2、 means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.2143 mL 11.0717 mL 22.1435 mL5 mM 0.4429 mL 2.2143 mL 4.4287 mL10 mM 0.2214 mL 1.1072 mL 2.2143 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使

3、，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.54 mM); Clear solution此案

4、可獲得 2.5 mg/mL (5.54 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemE此案可獲得 2.5

5、mg/mL (5.54 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.54 mM); Clear solution此案可獲得 2.5 mg/mL (5.54 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L

6、油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Cabergoline種麥衍的多巴胺 D2 亞類受體激動(dòng)劑，親和作于 D2，D3 和 5-HT2B 受體，Ki 分別為0.7，1.5 和 1.2。IC & Target Ki: 0.7 (Dopamine D2 receptor), 1.5 (Dopamine D3 receptor), 1.2 (5-HT2B receptor)1體外研究 Cabergoline acts as a potent agonist of D2, D3 and 5-HT2B receptors. Pretreatment with Cabergolin

7、e inhibits H2O2-induced neuronal cell death in a dose-dependent manner. In the following experiments, 10 M of Cabergoline is usedto investigate its neuroprotective effects. MAP2 staining reveals that Cabergoline significantly suppresses the loss ofneurons caused by H2O2 incubation. The detection of

8、apoptotic nuclear condensation suggested that Cabergolineprevents apoptotic cell death following H2O2 exposure1.體內(nèi)研究 Cabergoline has a longer elimination half-life (63 to 109 h) compared with other D2-like receptor agonists, both along-lasting clinical effect following single-dose administration, an

9、d an improvement in the quality of life of patientswith chronic diseases are expected1. The most significant reduction in rapid eye movement (REM) sleep boutnumber occurred during the light phase, in which Cabergoline-injected female handled mice has 67.3% less REMsleep bouts (F(1,11)=12.892, P=0.00

10、4) than Cabergoline-injected females that are restrained, although the greatestnumber 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) f

11、rom5.81.3 to 0.08 ng/mL within 2 hours of injection. After a 7-day recovery period, PRL levels return to values that arenot different from baseline (5.00.60 ng/mL; F(1,6)=0.715, P=0.43)2.PROTOCOLCell Assay 1 Primary cortical neurons are prepared. Cabergoline (10 M; except for experiments of dose-dep

12、endency) is appliedto cortical cells at DIV 6-7. After 24-hour Cabergoline treatment (except for examination of pretreatment time-dependency of Cabergoline), H2O2 (50 M; except for the dose-dependency of H2O2) is added. All inhibitors andantagonists, including spiperone, U0126, SB203580, SP600125, A

13、P5, and nifedipine are applied 20 min beforeCabergoline or H2O2 addition. L-glutamate is added at DIV 7-8 for cell death induction. Cell survival rate is measuredby MTT assay. After the indicated treatment with drugs is completed, culture medium is replaced with 200 L freshmedium containing 40 l MTT

14、 solution (2.5 mg/mL, diluted in PBS) and cells are incubated at 37C for 1.5-2.5 hours.Then, 200 L lysis buffer containing isopropyl alcohol is applied to each well and mixed by pipetting. Each sample ismoved to a 96-well plate and its absorbance at 570 nm is measured using an iMark Micro plate lead

15、er. Cell survivalrate is quantitated by absorbance measurement, because MTT (yellow) is deoxidized to formazan (violet) inproportion to mitochondrial activity1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Page 2 of 3 www.MedChemEAdministr

16、ation 2 Female and male C57BL/6J mice are used.Cabergoline is dissolved in 100% pharmasolve and then diluted with 20%-cyclodextrin in water to yield a final concentration of 0.15-0.5 mg/mL Cabergoline. Mice received a 0.3-mg/kg ipinjection of Cabergoline or vehicle. All drugs are prepared within 48

17、hours of experiment and stored at 4C. Solutionsare allowed to reach at room temperature before injection.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Nat Commun. 2020 Feb 18;11(1):941. Acta Pharmacol Sin. 2020 May 12.See more customer val

18、idations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. 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 sl