雌二醇作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetEstradiolCat. No.: HY-B0141CAS No.: 50-28-2分式: CHO分量: 272.38作靶點(diǎn): Estrogen Receptor/ERR; Endogenous Metabolite作通路: Others; Metabolic Enzyme/Protease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 : 50 mg/mL (183.57 mM)Ethanol : 20 mg/mL (73.43 mM

2、; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.6713 mL 18.3567 mL 36.7134 mL5 mM 0.7343 mL 3.6713 mL 7.3427 mL10 mM 0.3671 mL 1.8357 mL 3.6713 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：-

3、80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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% salineSol

4、ubility: 2.5 mg/mL (9.18 mM); Clear solution此案可獲得 2.5 mg/mL (9.18 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)Page 1 of 2 www.MedChemESolubility: 2.5 mg/mL (9.18 mM);

5、 Clear solution此案可獲得 2.5 mg/mL (9.18 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 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.18 mM); Clear solution此案可獲得 2.5 mg/mL (9.18 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

6、DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Estradiol 種類 醇性激素，對(duì)維持性的育能和第性征關(guān)重要。Estradiol 通過雌激素受體 (ER) 途徑上 調(diào) IL-6 表達(dá)123。IC & Target Human Endogenous Metabolite體外研究 Estradiol causes new dendritic spines and synapses in hippocampal CA1 pyramidal cells. Estradiol increases NMDAreceptor binding by 46%

7、in parallel with dendritic spine and synapse density. Estradiol also elevates sensitivity of CA1pyramidal cells to NMDA receptor-mediated synaptic input and such an effect is correlated with the estradiol-inducedincrease in dendritic spine density in the apical dendritic tree of these cells1. Estrad

8、iol reduces Ba2+ entry reversiblyvia Ca2+ channels in acutely dissociated and cultured neostriatal neurons. Estradiol also reduces Ba2+ currents but issignificantly less effective than Estradiol in rat neostriatal neurons2.體內(nèi)研究 Estradiol functions in hippocampal synapse density during the estrous cy

9、cle in the adult rat4. Estradiol reverses theovariectomy-induced decrease in spine density. Estradiol in combination with progesterone enhances spine densityfor 2 to 6 h but decreases following estradiol alone5.PROTOCOLCell Assay 3 Briefly, B9 cells (5103/well of a 96-well plate) are cultured with a

10、 series of dilutions of the supernatants in a finalvolume of 100 mL of RPMI 1640, supplemented with 510-5mol/Lof 2-mercaptoethanol, 10% FBS, 100 U/mLpenicillin, and 100 g/mL streptomycin in flat-bottom microtiter plates. After 42 h, 0.5 Ci of 3Hthymidine is added.6 h later, the cells are harvested a

11、nd the radioactivity incorporated is determined. IL-6 is quantitated from a standardcurve set up with known amounts of recombinant human or mouse IL-6. The anti-IL-6 monoclonal antibodycompletely inhibited the ability of the B9 cells to proliferate in response to recombinant mouse IL-6. In addition,

12、 wedetermined that B9 cells do not proliferate in response to IL-I or TNF, and that antibodies to these two cytokines didnot affect the cell proliferation in response to IL-6. Further, it is established that neither Estradiol (17-estradiol), northe 0.01% ethanol used as vehicle in these experiments,

13、 has any effect on the bioassay.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Adult female Sprague Dawley rats are housed on a 12 hr light/dark cycle with unlimited access to food and water.Administration 1 These animals are left gonadally inta

14、ct (intact), ovariectomized and treated with estradiol benzoate (OVX+E), orovariectomized and treated with sesame oil vehicle (OVX+O). The hormone treatment regimen that is used in theseexperiments has been shown previously to result in differences in CA1 pyramidal cell dendritic spine and synapsede

15、nsity. Six days before electrophysiological analysis, animals are ovariectomized under Metofane anesthesia usingaseptic surgical procedure. After surgery, animals are housed individually. On days 3 and 4 after surgery, OVX+EPage 2 of 3 www.MedChemEanimals are injected (s.c.) with 10 g of 17-estradio

16、l benzoate in 100 L of sesame oil vehicle; OVX+Oanimalsreceive oil vehicle at each injection time. Forty-eight hours after the second estradiol or vehicle injection,animals are killed by decapitation and hippocampal slices are prepared from their brains. Gonadally intact animalsare killed at random

17、stages of the estrous cycle.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) Hum Reprod. 2019 May 1;34(5):804-812. Cell Commun Signal. 2019 Aug 14;17(1):94. J Cell Mol Med. 2019 Nov 28. Biomed Pharmacother. 2019 May 25;116:109001.See more cus

18、tomer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Woolley CS, et al. Estradiol increases the sensitivity of hippocampal CA1 pyramidal cells to NMDA receptor-mediated synaptic input: correlation withdendritic spine density. J Neurosci. 1997 Mar 1;17(5):1848-59.2. Mermelstein PG, et al. Estradiol reduces calcium currents in rat neostriatal neurons via a membrane receptor. J Neurosci. 1996 Jan 15;16(2):595-604.3. Quanfu Huang, et al. 17-estradiol Upregulates IL6 Expression Through the ER Pathway to Promote Lung Adenocarcinoma Progression