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纳曲吲哚盐酸盐  ≥95%

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包装规格：5mg 10mg 25mg 50mg in glass bottle
溶解性：溶于DMSO(≥188mg/mL）
产品描述：基本信息 产品编号： N11385 产品名称： Naltrindole hydrochloride CAS: 111469-81-9   储存条件 粉末 -20℃ 四年     分子式： C26H27ClN2O3 溶于液体 -80℃ 6个月 分子量： 450.96 -20℃ 1个月 化学名：  22-(Cyclopropylmethyl)-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15,17,19(25)-heptaene-2,16-diol Solubility (25°C)：   体外:   DMSO   Ethanol   Water   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 2.2175mL 11.0875mL 22.1749mL 5mM 0.4435mL 2.2175mL 4.4350mL 10mM 0.2217mL 1.1087mL 2.2175mL   生物活性 产品描述 一种高效，选择性的非多肽类 δ opioid 受体拮抗剂，Ki值为0.02 nM。 靶点 Ki:0.02nM (δ opioid),64nM (μ opioid),66nM (κ opioid)   体外研究 Opioid drugs exert a wide spectrum of physiological and behavioral effects.These effects are mediated via membranebound receptors,of which the best characterized are the kappa,delta,and mu receptors.Naltrindole inhibits the proliferation of cultured human U266 MM cells in a time-and dose-dependent manner with an EC50 of 16μM.Treatment of U266 cells with naltrindole significantly decreases the level of the active,phosphorylated form of the kinases,extracellular signal-regulated kinase and Akt,which may be related to its antiproliferative activity.Naltrindole inhibits growth and induces apoptosis in the three characteristic SCLC cell lines,NCI-H69,NCI-H345,and NCI-H510.Naltrindole treatment reduces constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells and also its downstream effectors glycogen synthase kinase-3β and the Forkhead transcription factors AFX and FKHR. 体内研究 Naltrindole significantly decreases tumor cell volumes in human MM cell xenografts in severe combined immunodeficient mice.In mice, naltrindole at 20mg/kg s.c.antagonizes the δ-selective agonist effect of [D- Ser,Leu,Thr]enkephalin (DSLET) without blocking the antinociceptive effect of morphine or U50488H.Naltrindole is the only highly selective δ antagonist that is active upon peripheral administration.Acute naltrindole induces significant decreases in external and total ambulation (horizontal activity) and rearing behaviour (vertical activity),as well as a significant increase in grooming frequency.In animals chronically treated with naltrindole there is an increase in total ambulation one day after the discontinuation of the treatment.   推荐实验方法(仅供参考) 细胞实验:   U266 cells are plated in 96-well plates at 2000 cells per well in 100μL of RPMI 1640 medium,supplemented with 10% fetal bovine serum,100 U/mL penicillin,and 100μg/mL streptomycin sulfate.Cells are incubated in quadruplicate in the presence of the various antineoplastic agents to construct dose-response curves,alone or in combination with various doses of naltrindole.At the end of the incubation 10μL of WST-1 cell proliferation reagent is added to each well,and the plates are returned to the incubator for 1h.Absorbance is then measured.   动物实验:   Rats: Effects of neonatal naltrindole treatments on open field activity is tested in 20-day old rats.The animals are injected chronically with saline or naltrindole (1mg/kg,s.c.) (from birth to day 19),and 1 day after the discontinuation of this treatment are studied for the acute effects of naltrindole (1mg/kg,i.p.).
保存条件：-20℃

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