鹽酸脫氫紫堇堿作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetDehydrocorydaline chlorideCat. No.: HY-N0674ACAS No.: 10605-03-5分式: CHClNO分量: 401.88作靶點: p38 MAPK; Autophagy作通路: MAPK/ERK Pathway; Autophagy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 : 25 mg/mL (62.21 mM; Need ultrasonic)SolventMass1 mg 5 m

2、g 10 mgConcentration制備儲備液1 mM 2.4883 mL 12.4415 mL 24.8830 mL5 mM 0.4977 mL 2.4883 mL 4.9766 mL10 mM 0.2488 mL 1.2442 mL 2.4883 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In

3、 Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.22 mM); Clear solution此案可獲得 2.5 mg/mL (6.22 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25

4、.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 (6.22 mM); Clear solution此案可獲得 2.5 mg/mL (6.22 mM，飽和度未知) 的澄清溶液。Page 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

5、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 (6.22 mM); Clear solution此案可獲得 2.5 mg/mL (6.22 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。BIOLOGICAL ACTIVITY物活性 Dehydrocorydaline chloride 強(qiáng) p38 MAPK 的活化。種天然物堿類物質(zhì)，具有抗炎、

6、抗癌等功效。Dehydrocorydaline chloride 能夠增IC & Target p38 MAPK1體外研究 Treatment of C2C12 myoblasts with 500 nM Dehydrocorydaline increases the expression levels of muscle-specificproteins, including MyoD, myogenin and myosin heavy chain. Treatment with Dehydrocorydaline elevates p38 MAPKactivation and the i

7、nteraction of MyoD with an E protein. Furthermore, defects in differentiation-induced p38 MAPKactivation and myoblast differentiation induced by depletion of the promyogenic receptor protein Cdo in C2C12myoblasts are restored by Dehydrocorydaline treatment1. Dehydrocorydaline significantly inhibits

8、MCF-7 cellproliferation in a dose- dependent manner, which can be reversed by a caspase-8 inhibitor, Z-IETD-FMK.Dehydrocorydaline increases DNA fragments without affecting m. Western blotting assay shows thatdehydrocorydaline dose-dependently increases Bax protein expression and decreases Bcl-2 prot

9、ein expression.Furthermore, dehydrocorydaline induces activation of caspase-7,-8 and the cleavage of PARP without affectingcaspase-9. These results show that dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosismediated by regulating Bax/Bcl-2, activating caspases as well as clea

10、ving PARP3.體內(nèi)研究 Dehydrocorydaline (3.6, 6 or 10 mg/kg, i.p.) shows a dose-dependent antinociceptive effect in the acetic acid-inducedwrithing test and significantly attenuates the formalin-induced pain responses in mice. In the formalin test, dehydrocorydaline decreases the expression of caspase 6 (

11、CASP6), TNF-, IL-1 and IL-6 proteins in the spinal cord.These findings confirm that Dehydrocorydaline has antinociceptive effects in mice2.PROTOCOLCell Assay 3 Briefly, MCF-7 cells (1104 cells/well) are seeded in 96-well plates and treated with different concentrations ofdehydrocorydaline (0-200 M)

12、for 24 h. The cell viability is determined. To explore the role of caspase-8 indehydrocorydaline induced cytotoxicity, a caspase-8 inhibitor Z-IETD-FMK (10 M) is co-incubated with 200 Mdehydrocorydaline.MCE has not independently confirmed the accuracy of these methods. They are for reference only.An

13、imal Briefly, the mice are placed individually in glass beakers and are allowed to acclimate for 30 min before the test. TheAdministration 2 vehicle or Dehydrocorydaline (3.6, 6 or 10 mg/kg) are injected (10 ml/kg, i.p.) 15 min prior to the formalin injection.Morphine (10 mg/kg) or diclofenac sodium

14、 (20 mg/kg) are injected 15 and 30 min, respectively, prior to the formalininjection as positive controls. Then, 25 L of a 5% formalin solution is injected into the plantar surface of the righthind paw of each mouse. Immediately after the formalin injection, the mice are placed individually in the b

15、eakers, anda mirror is placed under the beaker to allow clear observation of the paws of the animals. The time that the animalsspent on biting/licking the injected paw is measured with a stopwatch every 5 min and considered as indication ofnociception.Page 2 of 3 www.MedChemEMCE has not independentl

16、y 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) J Cell Physiol. 2019 May 15. J Nutr. 2020 May 9. pii: nxaa128. Biochem Biophys Res Commun. 2018 Sep 5;503(2):467-473. Biochem Biophys Res Commun. 2018 May 23;499(4):743-750. J Clin Neurosci. 2020 Apr 30. pii: S0967-58

17、68(19)31066-5.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Yoo M, et al. Dehydrocorydaline promotes myogenic differentiation via p38 MAPK activation. Mol Med Rep. 2016 Oct;14(4):3029-36.2. Yin ZY, et al. Antinociceptive effects of dehydrocorydaline in mouse models of inflammatory pain involve the opioid receptor and inflammatorycytokines. Sci Rep. 2016 Jun 7;6:271293. Xu Z, et al. Dehydrocorydaline inhibits breast cancer cells proliferation by inducing apoptosis in