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Sofiniclin  ≥95%

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包装规格：1mg in glass bottle
溶解性：溶于DMSO(7mg/ml 超声）
产品描述：基本信息 产品编号： S10967  产品名称： Sofiniclin CAS: 799279-80-4   储存条件 粉末 -20℃ 四年     分子式： C10H11Cl2N3 溶于液体 -80℃ 6个月 分子量： 244.12 -20℃ 1个月 化学名：  (1s,5s)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3.2.0]heptane 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 4.0963mL 20.4817mL 40.9635mL 5mM 0.8193mL 4.0963mL 8.1927mL 10mM 0.4096mL 2.0482mL 4.0963mL   生物活性 产品描述 一种nAChR的激动剂，作为注意力缺陷症的潜在的非刺激性研究。 靶点 nAChR 体外研究 Sofiniclin is more potent than ABT-089 at both receptor subtypes,with Ki values of 1.9nM for 125I-α-conotoxinMII binding and of 1.3nM for 125I-epibatidine binding. 体内研究 Sofiniclin (0.001 to 0.10mg/kg,p.o.) produces significant reductions in LIDs compared to vehicle monkey.Sofiniclin (0.1mg/kg) does not decrease LIDs in monkeys with severe nigrostriatal damage.   推荐实验方法(仅供参考) 激酶实验： Receptor studies with ABT-089 and Sofiniclin are done using rat striatal sections.α6β2* nAChR levels are assayed using 125Iα-conotoxinMII (α-CtxMII) (specific activity,2200 Ci/mmol).α4β2* nAChRs are measured by determining the binding of 125Iepibatidine (specific activity,2200 Ci/mmol) in the presence of 100nM α-CtxMII to block α6β2* nAChRs. After assay,sections are exposed to Kodak MR film.To evaluate binding, optical density readings are converted fmol/mg tissue using 125Istandards.   动物实验:   Monkeys:Once stable dyskinesias develops,the effects of ABT-089 and Sofiniclin are determined on LIDs.For these studies,there are two sets of MPTP-lesioned monkeys,Set A (n=17) and Set B (n=16).Set A monkeys have previously been treated with nicotine and/or nAChR drugs,followed by a 10 week ishout period (nAChR drug-primed).Set B monkeys have not received any nAChR drug when ABT-089 treatment is initiated (nAChR drug-naive).Our rationale for the use of these two sets of monkeys is to determine if prior treatment with nAChR drugs altered their ability to decrease LIDs.For both sets,there are 3 experimental groups of monkeys,a vehicle-treated group (n=6),a nAChR drug-treated group (n=5 or 6) and a nicotine-treated group (n=5),as a positive control.The monkeys are assigned to the groups such that there are similar number of males and females,with comparable average LID scores.
保存条件：-20℃

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