鹽酸青藤堿作用機制 - Medchemexpress - MCE中國

1、Product Data SheetSinomenine hydrochlorideCat. No.: HY-15122ACAS No.: 6080-33-7分式: CHClNO分量: 365.85作靶點: NF-B; Opioid Receptor; Autophagy; Apoptosis作通路: NF-B; GPCR/G Protein; Neuronal Signaling; Autophagy; Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO :

2、 100 mg/mL (273.34 mM; Need ultrasonic and warming)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.7334 mL 13.6668 mL 27.3336 mL5 mM 0.5467 mL 2.7334 mL 5.4667 mL10 mM 0.2733 mL 1.3667 mL 2.7334 mL請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C

3、儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.83 mM); Clea

4、r solution此案可獲得 2.5 mg/mL (6.83 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. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.83 mM); Clear solution此案可獲得 2.5 mg/mL (6.83 mM，飽和度未知) 的澄清溶液。Page

5、1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.83 mM); Clear solution此案可獲得 2.5 mg/mL (6.83 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICA

6、L ACTIVITY物活性 Sinomenine hydrochloride (Cucoline hydrochloride) 來 Sinomenium acutum 的種物堿，是NF-B 活化的阻斷 劑1。Sinomenine 也 阿受體 (-opioid receptor) 激活劑2。IC & Target NF-B -opioid receptor體外研究 Cell viability is gradually decreased with increasing Sinomenine hydrochloride concentration. The migration ability o

7、fMDA-MB-231 cells is significantly weakened by 0.25, 0.5, and 1 mM of Sinomenine hydrochloride treatment. Thewound-healing assay reveals that 0.25 and 0.5 mM Sinomenine hydrochloride significantly suppress the healing ofthe wound. When the MDA-MB-231 cells are treated with 0.5 mM Sinomenine hydrochl

8、oride, the healing progress isabout 50%, but in the group treated with 0.25 mM Sinomenine hydrochloride and the untreated control, the healingis about 80% and nearly 95%, respectively. The IB assay following inhibitor of NF-B (IB) antibody IP shows that thebinding of NF-B to IB is inhibited by Sinom

9、enine hydrochloride treatment in a dose-dependent manne1.體內研究 Sinomenine hydrochloride (i.p.) produces antinociception in the hot plate and tail flick tests in male rats at 40 mg/kg,but not at lower doses (10 or 20 mg/kg). At 10 to 40 mg/kg Sinomenine hydrochloride does not produce anyobservable sid

10、e effect such as sedation, allergy or motor impairments. At 80 mg/kg, Sinomenine hydrochloride ismildly sedative in rats. Sinomenine hydrochloride at 80 mg/kg i.p. does not produce any observable side effects inmice. I.p or p.o. Sinomenine hydrochloride at 40 or 80 mg/kg dose-dependently reduces mec

11、hanical hypersensitivityin nerve injured mice. I.p. Sinomenine hydrochloride at 40 mg/kg, but not lower doses or vehicle, significantlydecreases mechanical and cold allodynia for up to 240 min without producing motor deficits or sedation3. At dosesof 10 to 40 mg/kg, Sinomenine hydrochloride dose-dep

12、endently increases the paw withdrawal threshold. In non-chronic constriction injury (CCI) healthy rats, Sinomenine hydrochloride at the dose range of 10 to 40 mg/kg does notchange the immobility behavior in the forced swimming test4.PROTOCOLCell Assay 1 The MDA-MB-231 human triple negative and 4T1 m

13、ouse breast cancer cell lines are used in this study. For theexperiments, the cells are grown in 24-well plates at 3.5104 cells/well. Following incubation for 24 or 48 h inmedium containing different concentrations of Sinomenine hydrochloride, proliferation of the cells are detected withCell Countin

14、g Kit-8 solution according to the manufacturers instructions1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male Sprague-Dawley rats weighing of 250 to 300 g are used in this experiment. For the duration of action of acuteAdministration 4 Sinom

15、enine hydrochloride study, different doses of Sinomenine hydrochloride (10 to 40 mg/kg) are administered 1day after surgery and then paw withdrawal threshold is measured every 30 min for 4 hours. For the study involvingdaily Sinomenine hydrochloride treatment, mechanical hyperalgesia measure is perf

16、ormed 3 h after daily drugtreatment. For antagonist studies, antagonists are given 10 min prior to 40 mg/kg Sinomenine hydrochlorideadministration4.Page 2 of 3 www.MedChemEMCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻 Free Radic Biol Med.

17、2018 Jun 2;124:205-213.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Song L, et al. Sinomenine inhibits breast cancer cell invasion and migration by suppressing NF-B activation mediated by IL-4/miR-324-5p/CUEDC2 axis.Biochem Biophys Res Commun. 2015 Aug 28;464(3):7

18、05-10.2. Gao T, et al. Analgesic effect of sinomenine in rodents after inflammation and nerve injury. Eur J Pharmacol. 2013 Dec 5;721(1-3):5-11.3. Zhu Q, et al. Antinociceptive effects of sinomenine in a rat model of neuropathic pain. Sci Rep. 2014 Dec 1;4:7270.4. Wang MH, et al. Activation of opioid mu-receptor by sinomenine in cel