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Org 27569  ≥98%

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包装规格：10mg 50mg in glass bottle
溶解性：溶于DMSO（≥52.2 mg/mL）
产品描述：基本信息 产品编号： O10258 产品名称： Org 27569 CAS: 868273-06-7   储存条件 粉末 -20℃ 四年     分子式： C24H28ClN3O 溶于液体 -80℃ 6个月 分子量： 409.95 -20℃ 1个月 化学名：  5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide Solubility (25°C)：   体外:   DMSO 82mg/mL (200.02mM) Ethanol Insoluble Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.4393mL 12.1966mL 24.3932mL 5mM 0.4879mL 2.4393mL 4.8786mL 10mM 0.2439mL 1.2197mL 2.4393mL 50mM 0.0488mL 0.2439mL 0.4879mL 生物活性 产品描述 一种有效的 CB1 receptor 别构调节剂，既能增加激动剂与 CB1 结合，又能抑制激动剂诱导的 CB1 信号通路。 靶点 Cannabinoid Receptor   体外研究 Org 27569 enhances agonist (CP55940) binding,promotes agonist binding to CB1 yet inhibits agonist-induced G protein activation and blocks the agonist-induced conformational changes in TM6.Org 27569 inhibits agonist-induced TM6 movement in CB1 detected by a fluorescent probe on site 342.Org 27569 produces a significant,but saturable,increase in the level of specific [3H]CP 55,940 binding.Org 27569 (1μM) inhibits electrically evoked contractions of the mouse vas deferens with the pEC50 and Emax being 8.66±0.11 and 77% (95% confidence limits,70.6-82.7),respectively.In hCB1R cells,Org 27569 (1 and 10μM) behaves as a weak inverse agonist producing a small but significant decrease in basal [35S]GTPγS binding.Org 27569 is less effective as an inhibitor of WIN55212-mediated inhibition of forskolin-stimulated cAMP production.Org 27569 induces a small but significant level of ERK1/2 phosphorylation with an Emax of 19% and pEC50 value of 8.55±0.99. 体内研究 ORG 27569 (3.2 and 5.6 mg/kg, i.p.) significantly attenuates cocaine associated cue-induced reinstatement, cocaine priminginduced reinstatement, methamphetamine associated cue-induced reinstatement and methamphetamine priming-induced reinstatement in rat[1]. Org27569 (30mg/kg, i.p.) produces CB1-independent hypophagic effects and does not affect the discriminative stimulus effects of anandamide (AEA). Org27569 (100 μg intracerebroventricularly) does not affect the pharmacologic effects of systemically administered CP55,940 compared with vehicle. 推荐实验方法(仅供参考) 激酶实验： Binding assays are performed with the CB1 receptor agonist [3H]CP 55,940 (0.7nM) and the CB1 receptor antagonist [3H]SR 141716A (1.2nM),1mg/mL BSA and 50mM Tris buffer containing 0.1mM EDTA and 0.5mM MgCl2,pH 7.4,in a total assay volume of 500μL.Binding is initiated by the addition of mouse brain membranes (30μg).Assays are carried out at 37℃ for 60 min before termination by addition of ice-cold wash buffer (50mM Tris buffer and 1mg/mL BSA) and vacuum filtration using a 24-well sampling manifold and Whatman GF/B glass-fiber filters that have been soaked in wash buffer at 4℃ for 24h.Each reaction tube is washed five times with a 4-mL aliquot of buffer.The filters are oven-dried for 60 min and then placed in 5mL of scintillation fluid,and radioactivity is quantitated by liquid scintillation spectrometry.Specific binding is defined as the difference between the binding that occurs in the presence and absence of 1μM concentrations of the corresponding unlabeled ligand and is 70 to 80% of the total binding.   细胞实验:   细胞系 HEK293 浓度 ~10μM 处理时间 5到15分钟 方法 细胞表达CB1受体暴露于ORG27569（10μM）5〜15分钟。Fortoxin处理以消除Gi耦合作用，PTX以5纳克/毫升加入培养基。随后在毒素存在下培养18小时，细胞用PBS清洗两次，用化合物处理。细胞用冰预冷的PBS洗涤，细胞裂解物通过冰预冷的裂解缓冲液(150mM NaCl，1.0% IGEPAL CA-630，0.5%脱氧胆酸钠，0.1% SDS，以及50mM Tris，pH 7.5包含4-(2-氨乙基)苯磺酰氟，胃蛋白酶抑制剂A，E-64，苯丁抑制素，亮抑酶肽，以及抑肽酶作为蛋白酶抑制剂)处理获得。   动物实验:   Following a 1-week acclimation period,CB1 (+/+) and (−/−) mice are food-deprived,given an intraperitoneal injection of Org27569 (30mg/kg),rimonabant (10mg/kg;positive control),or vehicle at 23h,and placed in a plastic cage with access to water.A premeasured amount (2.3-2.6g) of sweet cereal or standard chow is placed in the test cage from 24 to 26h.All mice receive each treatment condition in a counterbalanced design,with at least 96h between test days.
保存条件：-20℃

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