SB-277011 hydrochloride ≥98%
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| 包装规格: | 5mg 10mg 25mg 50mg in glass bottle |
| 溶解性: | 溶于水(16.67mg/mL 超声),溶于DMSO(50mg/mL 超声) |
| 产品描述: | 基本信息 产品编号: S10826 产品名称: SB-277011 hydrochloride CAS: 215804-67-4 储存条件 粉末 -20℃ 四年 分子式: C28H30N4O.HCl 溶于液体 -80℃ 6个月 分子量: 475.02 -20℃ 1个月 化学名: N-[4-[2-(6-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]quinoline-4-carboxamide;hydrochloride 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 2.1052mL 10.5259mL 21.0517mL 5mM 0.4210mL 2.1052mL 4.2103mL 10mM 0.2105mL 1.0526mL 2.1052mL 生物活性 产品描述 一种强效、选择性、口服生物利用度和脑透多巴胺 D3 受体(D3R) 拮抗剂,其 Ki 值在啮齿动物和人D3R 分别为 10.7nM 和 11.2nM。 靶点 Dopamine Receptor 5-HT Receptor 体内研究 SB-277011 hydrochloride has an excellent pharmacokinetic profile,exhibits oral bioavailability 43%,half-life:2.0h,plasma clearance 19mL/min/kg) and to be highly brain-penetrant (brain:blood ratio of 3.6:1),with a clean P450 profile in the rat.SB-277011 hydrochloride (SB 277011;3mg/kg,p.o.) completely reverses the effects of quinelorane in the nucleus accumbens,but does not reverse the effects of quinelorane in the striatum at 93mg/kg in rats.SB-277011 (intraperitoneal injection;12.5-25mg/kg) significantly and dose-dependently reduces intravenous cocaine selfadministration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats.When it increases to 50mg/kg,SB-277011 can significantly inhibit basal and cocaine-enhanced locomotion in rats. |
| 保存条件: | -20℃ |
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