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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDehydrocorydaline chlorideCat. No.: HY-N0674ACAS No.: 10605-03-5Synonyms: 13-Methylpalmatine chloride分式: CHClNO分量: 401.88作靶點: p38 MAPK作通路: MAPK/ERK Pathway儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性
2、數(shù)據(jù)體外實驗 DMSO : 25 mg/mL (62.21 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration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,并請注意儲備液的保存式和期限。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)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟海僖来翁砑又軇?為保證實驗結(jié)
3、果的可靠性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當(dāng)天使;澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):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 solution2. 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 solution3. 請依序添加每種溶劑: 10% DMSO 90% co
4、rn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.22 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Dehydrocorydaline chloride種天然物堿類物質(zhì),具有抗炎、抗癌等功效。Dehydrocorydalinechloride 能夠增強 p38 MAPK 的活化。IC50 & Target p38 MAPK 1體外研究 Treatment of C2C12 myoblasts with 500 nM Dehydrocorydali
5、ne increases the expression levels of muscle-specific proteins, including MyoD, myogenin and myosin heavy chain. Treatment with Dehydrocorydalineelevates p38 MAPK activation and the interaction of MyoD with an E protein. Furthermore, defects indifferentiation-induced p38 MAPK activation and myoblast
6、 differentiation induced by depletion of thepromyogenic receptor protein Cdo in C2C12 myoblasts are restored by Dehydrocorydaline treatment 1.Dehydrocorydaline significantly inhibits MCF-7 cell proliferation in a dose- dependent manner, which can bereversed by a caspase-8 inhibitor, Z-IETD-FMK. Dehy
7、drocorydaline increases DNA fragments withoutaffecting m. Western blotting assay shows that dehydrocorydaline dose-dependently increases Baxprotein expression and decreases Bcl-2 protein expression. Furthermore, dehydrocorydaline inducesactivation of caspase-7,-8 and the cleavage of PARP without aff
8、ecting caspase-9. These results show thatdehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2,activating caspases as well as cleaving PARP 3.體內(nèi)研究 Dehydrocorydaline (3.6, 6 or 10 mg/kg, i.p.) shows a dose-dependent antinociceptive effect in the ac
9、eticacid-induced writhing test and significantly attenuates the formalin-induced pain responses in mice. In theformalin test, dehydrocorydaline decreases the expression of caspase 6 (CASP6), TNF-, IL-1 and IL-6proteins in the spinal cord. These findings confirm that Dehydrocorydaline has antinocicep
10、tive effects in mice2.PROTOCOLCell Assay 3 Briefly, MCF-7 cells (1104 cells/well) are seeded in 96-well plates and treated with different concentrationsof dehydrocorydaline (0-200 M) for 24 h. The cell viability is determined. To explore the role of caspase-8 indehydrocorydaline induced cytotoxicity
11、, a caspase-8 inhibitor Z-IETD-FMK (10 M) is co-incubated with 200M dehydrocorydaline.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Briefly, the mice are placed individually in glass beakers and are allowed to acclimate for 30 min before theAdm
12、inistration 2 test. The vehicle or Dehydrocorydaline (3.6, 6 or 10 mg/kg) are injected (10 ml/kg, i.p.) 15 min prior to theformalin injection. Morphine (10 mg/kg) or diclofenac sodium (20 mg/kg) are injected 15 and 30 min,respectively, prior to the formalin injection as positive controls. Then, 25 L
13、 of a 5% formalin solution isinjected into the plantar surface of the right hind paw of each mouse. Immediately after the formalin injection,the mice are placed individually in the beakers, and a mirror is placed under the beaker to allow clear2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEobserva
14、tion of the paws of the animals. The time that the animals spent on biting/licking the injected paw ismeasured with a stopwatch every 5 min and considered as indication of nociception.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 J Cell Ph
15、ysiol. 2019 May 15. Biochem Biophys Res Commun. 2018 Sep 5;503(2):467-473. Biochem Biophys Res Commun. 2018 May 23;499(4):743-750.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Yoo M, et al. Dehydrocorydaline promotes myogenic differentiation via p38 MAPK activation. Mol Med R
16、ep. 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 andinflammatory cytokines. Sci Rep. 2016 Jun 7;6:271293. Xu Z, et al. Dehydrocorydaline inhibits breast cancer cells proliferation by inducing apoptosis in MCF-
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