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L-771688  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： L10418 产品名称： L-771688 CAS: 200050-59-5   储存条件 粉末 -20℃ 四年 分子式： C28H33F2N5O5 溶于液体 -80℃ 二年 分子量： 557.59     化学名：  methyl(S)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-3-((3-(4-(pyridin-2-yl)piperidin-1-yl)propyl)carbamoyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate 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。   生物活性 产品描述 一个选择性 α1A-Adrenoceptor 受体拮抗剂，Ki 值为 0.43±0.02nM。 靶点 Ki:0.43±0.02nM (α1A-Adrenoceptor)   体外研究 Specific [3H]L-771688 binding to cloned human α1A-Adrenoceptors is inhibited with high potency by subtype selective compounds,GG818 (Ki=0.026±0.002nM) and L-771688 (Ki=0.052±0.008nM) and subtype non-selective α1-adrenoceptor antagonists,prazosin (Ki=0.088±0.0.032nM) and terazosin (Ki=1.8±0.65nM).The relative amount of [3H]L-771688 (0.5nM) binding in various rat tissue membranes is highest in submaxillary gland (9.5 pmol/g tissue),followed by brain (5.8 pmol/g tissue),vas deferens (4.3 pmol/g tissue),kidney (3.4 pmol/g tissue),heart (1.5 pmol/g tissue),urethra (1.1 pmol/g tissue) and prostate (0.88 pmol/g tissue).In contrast,low specific [3H]L-771688 binding is observed in rat urinary bladder (0.55 pmol/g tissue),liver (0.44 pmol/g tissue),aorta (0.11 pmol/g tissue) and spleen (0.11 pmol/g tissue).   推荐实验方法(仅供参考) 细胞实验:   [3H]L-771688 is prepared by a catalytic reduction of the precursor,L-797429,in the presence of tritium gas followed by preparative high pressure liquid chromatography.Receptor membranes are prepared for [3H]prazosin/[125I]HEAT binding assays.To measure [3H]L-771688 binding,980μL of membranes (cloning human α1A or rat tissues) are added to triplicate tubes containing 10μL of dimethyl sulfoxide (DMSO) (for total binding) or phentolamine (10μM final concentration,for nonspecific binding) or tested compounds (at the desiring final concentrations) and 10μL of [3H]L-771688 (0.3 to 0.6nM final concentration for routine studies and 10pM to 5nM for saturation assays).[3H]L-771688 is diluted in DMSO/methanol/water (1:1:2) from stock solution to minimize its loss to the wall of test tubes.The binding reaction is conducted at 25℃ for 1h or various time intervals in the association rate studies.
保存条件：-20℃

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