去氢骆驼蓬碱作用机制 - Medchemexpress - MCE中国

1、Product Data SheetHarmineCat. No.: HY-N0737ACAS No.: 442-51-3分式: CHNO分量: 212.25作靶点: DYRK; 5-HT Receptor作通路: Protein Tyrosine Kinase/RTK; GPCR/G Protein; Neuronal Signaling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 : 30 mg/mL (141.34 mM)H2O : 0.1 mg/mL (insol

2、uble)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 4.7114 mL 23.5571 mL 47.1143 mL5 mM 0.9423 mL 4.7114 mL 9.4229 mL10 mM 0.4711 mL 2.3557 mL 4.7114 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

3、 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 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 (11.78 mM); Clear sol

4、ution此案可获得 2.5 mg/mL (11.78 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 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% corn oilSolubility: 2.5 mg/mL (11.78 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (11.78 mM，饱和度未知) 的澄

5、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 Harmine 种具有抗癌和抗炎活性的天然双特异性酪氨酸磷酸化调节激酶 (DYRK) 抑制剂。Harmine 对 5-HT2A 清 素受体具有亲和，Ki 值为 397 nM。IC & Target DYRK1A 5-HT2A Receptor397 nM (Ki)体外研究 Harmine inhibits tau phosphorylation by DYRK1A by selected

6、DANDYs, with an IC50 of 190 nM2.Harmine negativelyregulates homologous recombination (HR) by interfering Rad51 recruitment, resulting in severe cytotoxicity inhepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedly sensitizes Hep3B cells to the anti-proliferative effectsof Harmine3.体内研究 It is sh

7、own that brain water content is significantly increased in the TBI group. Treatment with Harmine significantlyreduces the tissue water content at 1, 3 and 5 days, compared with the TBI group. Harmine treatment significantlyreduces the escape latency at 3 and 5 days, compared with the TBI group. Post

8、-TBI administration of Harminesignificantly improves the motor function recovery of the rats at 1, 3 and 5 days following TBI, compared with the TBIgroup without Harmine treatment. The neuronal survival rate in the Harmine-treated group is significantly increased,compared with the TBI group. Adminis

9、tration of Harmine results in marked elevation in the expression of GLT-1,compared with the TBI group. The administration of Harmine significantly reduces the expression of caspase 3,compared with the TBI group4.PROTOCOLAnimal Rats4Administration 4 A total of 150 male Sprague-Dawley rats (age, 10-12

10、 weeks; weighing, 280-320 g; are used in the present study. Therats are randomly divided into three groups: Sham-operated group (sham; n=15); the TBI group (TBI; n=35) and theTBI + Harmine-treated group (Harmine; n=35). Harmine is administered immediately following TBI (i.p, 30 mg/kgper day) for up

11、to 5 days. The sham and TBI groups receive equal volumes of 0.9% saline solution (i.p.). The rats aregrouped as follows for examination of behavioral recovery: Sham, n=3; TBI, n=7; and Harmine, n=7. Following TBI,the NSS is evaluated at 1, 3 and 5 days. Each rat is assessed by an observer who is bli

12、nded to the animal treatment4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Cell Mol Med. 2019 Aug 27. Prog Neuropsychopharmacol Biol Psychiatry. 2017 Jun 15;79(Pt B):258-267. Sci Rep. 2015 Aug 3;5:12728. Onco Targets Ther. 2019 Jun 12;1

13、2:4585-4593.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Glennon RA, et al. Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A), dopamine (D(2) and benzodiazepine receptors.Drug Alcohol Depend. 2000 Aug 1;60(2):

14、121-32.2. Neumann F, et al. DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives. Sci Rep.2018 Feb 12;8(1):2859.3. Zhang L, et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells. Cancer Biol Ther. 2015;16(11):1585-92.4. Zhong Z, et al. Treatment with harmine ameliorates functional impairment and neuronal death following traumatic brain injury. Mol Med Rep. 2015Dec;12(6):7985-91.Mc