Product Data?SheetAlarelin AcetateCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-1740579561-22-1C??H??N??O??1287.42GNRH ReceptorGPCR/G ProteinPowderIn solvent-20°C-80°C-20°C3 years6 months1 monthInhibitors?Agonists?Screening Libraries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)Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM0.7767 mL0.1553 mL0.0777 mL3.8837 mL0.7767 mL0.3884 mL7.7675 mL1.5535 mL0.7767 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：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 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，澄清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?是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 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-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.MedChemExpress.cn
以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合均匀。
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) 的澄清溶液，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 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。
BIOLOGICAL ACTIVITY
?物活性体外研究
Alarelin acetate是合成的GnRH激动剂。
The cell viability in the presence of alarelin was significantly lower than that in the absence of alarelin. The maximum stimulatory effect on cell viability was achieved at a concentration of 10-5 M and it acted in a dose-dependent manner
[1]
体内研究
Alarelin could inhibit the gastric acid secretion both by direct actions on parietal cells in rats and by inhibiting vagous function[2]. Alarelin could significantly enhance ratio of G1 phase and decrease ratio of S phase of GSMC of rats[1].
PROTOCOL
Cell 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 24 h to approximately 800 g/L subconfluent state, 0.1 mL medium containing 2.5% calf serum and various
concentrations (0.001, 0.1, 10 μM) of alarelin is added to each well, respectively, and incubated for 24 h in a CO2 incubator. Each concentration is tested in at least 12 wells. Briefly, 15 μL of MTT solution is added to each well and incubated for 4 h. Then, the medium and MTT are removed and 150 μL of DMSO is added to each well and shaken for 10 min to dissolve the crystal. The OD is determined at 490 nm using an ELISA reader[1].MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal
Administration [2]
Rats: Male Sprague-Dawley rats are divided into two groups. In Group I: Gastric acid secretion is measured in a chambered stomach. Briefly, the abdomen is incised, and both the stomach and duodemun are exposed and tied respectively; then 1.5 mL 0.9% sodium chloride (containing Alarelin, 2 μg/kg) is infused into the each chambered stomach. After 15, 30, 45, 60 min, the gastric juice is drew out of the chambered stomach and the pH is measured in the ABL-500 respectively. The control is infused saline instead of Alarelin. In Group II: After anaesthetized, 2 mL Alarelin (2 μg/kg) is administered into the tail vein. The control is injected the saline instead of Alarelin. Then, the stomach and duodenum are tied and infused 1.5 mL saline immediately. After 15, 30, 45, 60 min, the gastric juice is also drew out of the chambered stomach and the pH is measured in the ABL-500 respectively[2].MCE has not independently confirmed the accuracy of these methods. They are for reference only.
REFERENCES
[1].?Chen L, et al. Expression of gonadotropin-releasing hormone receptor and effect of gonadotropin-releasing hormone analogue on proliferation of cultured gastric smooth 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 of rats. Life Sci. 2005 Feb 4;76(12):1351-65.
Page 2 of 3 www.MedChemExpress.cn
McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: tech@MedChemExpress.cn
Master of Small Molecules — 您?边的抑制剂?师
Page 3 of 3 www.MedChemExpress.cn
相关推荐：
loading