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1、Product Data SheetDehydrocorydaline chlorideCat. No.: HY-N0674ACAS No.: 10605-03-5分式: CHClNO分量: 401.88作靶点: p38 MAPK; Autophagy作通路: MAPK/ERK Pathway; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25 mg/mL (62.21 mM; Need ultrasonic)SolventMass1 mg 5 m
2、g 10 mgConcentration制备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;旦配成溶液,请分装保存,避免反复冻融造成的产品失效。储备液的保存式和期限:-80C, 6 months; -20C, 1 month。-80C 储存时,请在 6 个内使,-20C 储存时,请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In
3、 Vitro 式配制澄清的储备液,再依次添加助溶剂:为保证实验结果的可靠性,澄 的储备液可以根据储存条件,适当保存;体内实验的作液,建议您现现配,当天使; 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.22 mM); Clear solution此案可获得 2.5 mg/mL (6.22 mM,饱和度未知) 的澄清溶液。以 1 mL 作液为例,取 100 L 25
4、.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中,混合均匀;向上述体系中加50 L Tween-80,混合均匀;然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.22 mM); Clear solution此案可获得 2.5 mg/mL (6.22 mM,饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例,取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900
5、L 20% 的 SBE-CD 理盐溶液中,混合3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.22 mM); Clear solution此案可获得 2.5 mg/mL (6.22 mM,饱和度未知) 的澄 溶液,此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例,取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中,混合均匀。BIOLOGICAL ACTIVITY物活性 Dehydrocorydaline chloride 强 p38 MAPK 的活化。种天然物碱类物质,具有抗炎、
6、抗癌等功效。Dehydrocorydaline chloride 能够增IC & Target p38 MAPK1体外研究 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.体内研究 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.户使本产品发表的科研献 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
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