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SKF89976A hydrochloride  ≥98%

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包装规格：5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO（100 mg/mL 超声)
产品描述：基本信息 产品编号： S10540 产品名称： SKF89976A hydrochloride CAS: 85375-15-1   储存条件 粉末 -20℃ 四年     分子式： C22H25NO2 溶于液体 -80℃ 6个月 分子量： 335.45 -20℃ 1个月 化学名：  1-(4,4-Diphenylbut-3-en-1-yl)piperidine-3-carboxylic acid 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 2.6889mL 13.4445mL 26.8889mL 5mM 0.5378mL 2.6889mL 5.3778mL 10mM 0.2689mL 1.3444mL 2.6889mL   生物活性 产品描述 一种选择性GABA转运蛋白GAT-1抑制剂 靶点 IC50:0.28μM (GAT-1),137.34μM (GAT-2),202.8μM (GAT-3)   体外研究 SKF89976A has a weak antiallodynic action.SKF89976A weakly inhibits serotonin transporter (SERT),noradrenaline transporter (NET),and dopamine transporter (DAT) in chinese hamster ovary (CHO) cells stably expressing each transporter using a substrate uptake assay,with IC50 values of 3514,202.13,and 728.8,respectively.SKF89976A is a GABA-transport blocker.GABA (1mM) elicited an inward current that is completely suppressed by the GABA transport inhibitors tiagabine (10μM) and SKF89976A (100μM),but is unaffected by 100μM picrotoxin.100μM SKF 89976-A is known to block the transport of GABA into cells,completely eliminated the GABA-elicited current in a reversible fashion.SKF89976A is a nontransportable blockers of GAT-1.SKF89976-A also suppresses baseline inward currents that likely result from tonic GAT activation by background GABA.SKF89976A (100μM) reversibly reduces GAT currents in every studied cell by 67.9±4.4% (n=19).Intracellular perfusion of 20μM SKF89976-A progressively reduced and blocked GABA-induced GAT currents without blocking GABAAR-mediated currents (n=4). 体内研究 SKF89976A produces a weak antiallodynic response when administered i.v.(0.3mg/kg).The i.t.injection of SKF89976A dosedependently ameliorates the reduction in the withdrawal threshold in PSL model mice.   推荐实验方法(仅供参考) 细胞实验:   CHO cells stably expressing the mouse GAT subtypes,rat serotonin transporter (SERT),rat noradrenaline transporter (NET),and rat dopamine transporter (DAT) are incubated with 10nM tritium-labeled GABA or monoamines for 10 min in the absence or presence of various concentrations of the GAT inhibitors (e.g.,SKF89976A) tested.Values presented for SERT,NET,and DAT are the mean±S.E.M.for 3 experiments,with each being performed in duplicate.   动物实验:   Mice 5-week-old ddY male mice,weighing 25-30g at the beginning of the study are used.Mice are administered NNC05-2090,SKF89976A (0.3mg/kg,i.p.),(S)-SNAP5114,or amitriptyline.The composition of ACSF (in mM) is 142mM NaCl,5mM KCl,2mM CaCl2,2mM MgCl2,1.25mM NaH2PO4,10mM d-glucose,10mM HEPES,and 0.05% fatty acid-free bovine serum albumin (pH 7.4).The intraperitoneal (i.p.) injection of drugs is administered in a volume of 0.1mL/10 g body weight.When given intravenously (i.v.),solutions are injected into the tail vein in a volume of 0.1mL/10g body weight.The head of a mouse is placed into a plastic cap and the body is held with one hand for an intrathecal (i.t.) injection.A 27-gauge needle attached to a Hamilton microsyringe is inserted into the subarachnoid space between the L5 and L6 vertebrae of the conscious mouse and 5mL of the drug solution is slowly injected.
保存条件：-20℃

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