6-巰基嘌呤作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data Sheet6-MercaptopurineCat. No.: HY-13677CAS No.: 50-44-2分式: CHNS分量: 152.18作靶點(diǎn): Nucleoside Antimetabolite/Analog; Autophagy; Endogenous Metabolite作通路: Cell Cycle/DNA Damage; Autophagy; Metabolic Enzyme/Protease儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protec

2、t from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 35.71 mg/mL (234.66 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 6.5712 mL 32.8558 mL 65.7117 mL5 mM 1.3142 mL 6.5712 mL 13.1423 mL10 mM 0.6571 mL 3.2856 mL 6.5712 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;

3、 -20C, 1 month (protect from light)。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?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% sa

4、lineSolubility: 2.5 mg/mL (16.43 mM); Clear solution此案可獲得 2.5 mg/mL (16.43 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% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (16.43 mM); Clear solutio

5、n此案可獲得 2.5 mg/mL (16.43 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 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。Page 1 of 2 www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (16.43 mM); Clear solution此案可獲得 2.5 mg/mL (16.43 mM，飽和度未知) 的澄 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

6、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 6-Mercaptopurine種嘌呤類似物， 內(nèi) 性嘌呤的拮抗劑且已被泛作抗病藥物和免疫抑制藥物。IC & Target Human Endogenous Metabolite(批量添加)體外研究 6-Mercaptopurine hydrate (6-MP) induces NR4A3 transcriptional activity 1.6- to 11-fold (P0.01) in a dose-responsivemanner. It is found tha

7、t 6-Mercaptopurine hydrate leads to a dose-dependent increase in NR4A3 protein levels. 6-MPtreatment increases cell surface GLUT4 in both basal cells 1.8- to 3.6-fold (P0.01) and insulin-stimulated cells 2.9- to4.4-fold (P0.01) over that in controls. It is also found that 6-Mercaptopurine hydrate in

8、creases phospho-AS160significantly in a dose-responsive manner under both basal and insulin-stimulated conditions2.體內(nèi)研究 In the fetal telencephalons of the 6-Mercaptopurine hydrate (6-MP)-treated group, the S phase cell populationincreases at 36 and 48 h and returns to the control level at 72 h after

9、 treatment. The G2/M phase cell populationbegins to increase at 24 h, peaks at 36 h, decreases at 48 h, and finally returnes to the control level at 72 h. On theother hand, the sub-G1 phase cell population (apoptotic cells) begins to increase at 36 h, peaks at 48 h, and thendecreases at 72 h3.PROTOC

10、OLKinase Assay 2 L6 myotubes are treated with DMSO control or 6-Mercaptopurine hydrate (6-MP) for 24 h, with the final 3 h ofincubation including treatments in serum-free DMEM, and further incubated in the absence or presence of 100 nMinsulin for 60 min at 37C. Then, protein lysates (50 g) are colle

11、cted and subjected to SDSand immunoblottedwith primary antibodies against overnight at 4C. The proteins are finally quantified by densitometric analysis ofscanned films using Image J software2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2

12、 Cell viability is measured using Cell Viability Assay. L6 skeletal muscle cells are seeded in 96-well plates at a density of10,000 cells/well and differentiated into myotubes within 7 days. Cells are treated with different doses of 6-Mercaptopurine hydrate (6-MP) for 24 h before the assay. For anal

13、ysis of cell viability, plates are equilibrated at roomtemperature for 30 min; 50 L of Cell Titer-Glo reagent is added to each well, and plates are mixed for 12 min on anorbital shaker. Luminescence is quantified using a luminometer2.MCE has not independently confirmed the accuracy of these methods.

14、 They are for reference only.Animal Around thirteen-week-old pregnant rats are used in this study. The animals are housed individually in wire-meshAdministration cages in an air-conditioned room (temperature, 233C; humidity, 5020%; ventilation, 10 times/hour; lighting, 12 hlight to12 h dark cycle) a

15、nd are given pelleted diet and water ad libitum. In the experiment, fifteen pregnant rats areinjected i.p. with 50 mg/kg 6-Mercaptopurine hydrate (6-MP) on E13, and three dams each are sacrificed byexsanguination from the abdominal aorta under ether anesthesia at 12, 24, 36, 48, and 72 h. Fetuses ar

16、e collectedfrom each dam by Caesarean section. As controls, fifteen pregnant rats are injected i.p. with 2.0% methylcellulosesolution in distilled water at E13, and three dams are sacrificed at each of the same time-points3.Page 2 of 3 www.MedChemEMCE has not independently confirmed the accuracy of

17、these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Aug;97(8):1183-1193. PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Sahasranaman S, et al. Clinical pharmacology and pharmacogenetics of thio

18、purines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67.2. Liu Q, et al. 6-Mercaptopurine augments glucose transport activity in skeletal muscle cells in part via a mechanism dependent upon orphan nuclearreceptor NR4A3. Am J Physiol Endocrinol Metab. 2013 Nov 1;305(9):E1081-92.3. Kanemitsu H, et al. 6-Mercaptopurine (6-MP) induces cell cycle arrest and apoptosis of neural progenitor cells in the developing fetal