醋酸阿拉瑞林作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAlarelin AcetateCat. No.: HY-17405CAS No.: 79561-22-1分式: CHNO分量: 1287.42作靶点: GNRH Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (77.67 mM; Need ultrasonic)H2O : 100 mg/mL (77.67 mM; Need ultrasonic)SolventMass1 mg

2、5 mg 10 mgConcentration制备储备液1 mM 0.7767 mL 3.8837 mL 7.7675 mL5 mM 0.1553 mL 0.7767 mL 1.5535 mL10 mM 0.0777 mL 0.3884 mL 0.7767 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 I

3、n 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 (1.94 mM); Clear solution此案可获得 2.5 mg/mL (1.94 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 2

4、5.0 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 (1.94 mM); Clear solution此案可获得 2.5 mg/mL (1.94 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 (1.94 mM); Clear solution此案可获得 2.5 mg/mL (1.94 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 Alarelin acetate是合成的GnRH激动剂。体外研究 The cell viability in

6、the presence of alarelin was significantly lower than that in the absence of alarelin. The maximumstimulatory effect on cell viability was achieved at a concentration of 10-5 M and it acted in a dose-dependent manner1体内研究 Alarelin could inhibit the gastric acid secretion both by direct actions on pa

7、rietal cells in rats and by inhibiting vagousfunction2. Alarelin could significantly enhance ratio of G1 phase and decrease ratio of S phase of GSMC of rats1.PROTOCOLCell Assay 1 The cells are trypsinized in a solution of 2.5 g/L trypsin and seeded in a 96-well plate. After the cells are grown for 2

8、4h to approximately 800 g/L subconfluent state, 0.1 mL medium containing 2.5% calf serum and variousconcentrations (0.001, 0.1, 10 M) of alarelin is added to each well, respectively, and incubated for 24 h in a CO2incubator. Each concentration is tested in at least 12 wells. Briefly, 15 L of MTT sol

9、ution is added to each well andincubated for 4 h. Then, the medium and MTT are removed and 150 L of DMSO is added to each well and shakenfor 10 min to dissolve the crystal. The OD is determined at 490 nm using an ELISA reader1.MCE has not independently confirmed the accuracy of these methods. They a

10、re for reference only.Animal Rats: Male Sprague-Dawley rats are divided into two groups. In Group I: Gastric acid secretion is measured in aAdministration 2 chambered stomach. Briefly, the abdomen is incised, and both the stomach and duodemun are exposed and tiedrespectively; then 1.5 mL 0.9% sodium

11、 chloride (containing Alarelin, 2 g/kg) is infused into the each chamberedstomach. After 15, 30, 45, 60 min, the gastric juice is drew out of the chambered stomach and the pH is measured inthe ABL-500 respectively. The control is infused saline instead of Alarelin. In Group II: After anaesthetized,

12、2 mLAlarelin (2 g/kg) is administered into the tail vein. The control is injected the saline instead of Alarelin. Then, thestomach and duodenum are tied and infused 1.5 mL saline immediately. After 15, 30, 45, 60 min, the gastric juice isalso drew out of the chambered stomach and the pH is measured

13、in the ABL-500 respectively2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chen L, et al. Expression of gonadotropin-releasing hormone receptor and effect of gonadotropin-releasing hormone analogue on proliferation ofcultured gastric smoo

14、th muscle cells of rats. World J Gastroenterol. 2004 Jun 15;10(12):1780-4.2. Chen L, et al. Distribution, cloning and sequencing of GnRH, its receptor, and effects of gastric acid secretion of GnRH analogue in gastric parietal cells ofrats. Life Sci. 2005 Feb 4;76(12):1351-65.Page 2 of 3 www.MedChemEMcePdfHeight