去氫駱駝蓬堿作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetHarmineCat. No.: HY-N0737ACAS No.: 442-51-3分式: CHNO分量: 212.25作靶點(diǎn): DYRK; 5-HT Receptor作通路: Protein Tyrosine Kinase/RTK; GPCR/G Protein; Neuronal Signaling儲(chǔ)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(shí)驗(yàn) 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制備儲(chǔ)備液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請(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?/p>

3、 6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.78 mM); Clear sol

4、ution此案可獲得 2.5 mg/mL (11.78 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(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.78 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (11.78 mM，飽和度未知) 的澄

5、溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Harmine 種具有抗癌和抗炎活性的天然雙特異性酪氨酸磷酸化調(diào)節(jié)激酶 (DYRK) 抑制劑。Harmine 對(duì) 5-HT2A 清 素受體具有親和，Ki 值為 397 nM。IC & Target DYRK1A 5-HT2A Receptor397 nM (Ki)體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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