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伊曲茶碱  ≥98%

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包装规格：10mg 50mg 250mg 1g in glass bottle
溶解性：溶于DMSO（25.33 mg/mL 超声，加热）
产品描述：基本信息 产品编号： I10307  产品名称： Istradefylline CAS: 155270-99-8   储存条件 粉末 2-8℃ 四年     分子式： C20H24N4O4 溶于液体 -80℃ 6个月 分子量： 384.43 -20℃ 1个月 化学名：  1H-Purine-2,6-dione,3,7-dihydro-1,3-diethyl-8-(2-(3,4-dimethoxyphenyl)ethenyl)-7-methyl-,(E)- Solubility (25°C)：   体外:   DMSO 6mg/mL (15.6mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 30% propylene glycol,5% Tween 80,65% D5W 30mg/mL ＜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 2.6013mL 13.0063mL 26.0125mL 5mM 0.5203mL 2.6013mL 5.2025mL 10mM 0.2601mL 1.3006mL 2.6013mL   生物活性 产品描述 一种有效的，选择性的，可口服的 adenosine A2A receptor 拮抗剂，在帕金森疾病模型试验中，Ki 值为 2.2nM。 靶点 Adenosine A2A receptor 2.2nM(Ki)   体外研究 Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with Ki of 2.2nM versus 150nM.Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes.Istradefylline binds to A1 receptor,A2A receptor,and A3 receptor in human with Kis of>287nM,9.12nM,and>681nM,respectively,50.9nM and 1.57nM for A1 receptor and A2A receptor in rat,105.02nM and 1.87nM for A1 receptor and A2A receptor in mouse,respectively. 体内研究 Istradefylline (3.3mg/kg,i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later.Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with an ED50 of 0.05mg/kg and 0.26mg/kg,respectively.Istradefylline is over 10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs.Istradefylline combined with L-dopa cuases potent effects on haloperidol-induced and reserpine-induced catalepsy.Istradefylline (10mg/kg,p.o.) results an increase in locomotor activity to approximately twice that of control and improves motor disability in MPTP-treated common marmosets.Istradefylline (10mg/kg,p.o.) in combination with SKF80723,quinpirole,or L-DOPA produces a significant additive effect on locomotor activity and improvement of motor disability but not dysKinesia.   推荐实验方法(仅供参考) 细胞实验:   A CHO cell line permanently expressing the human adenosine A1or A2A receptor is cultured in α-MEM supplemented with 10% (v/v) fetal bovine serum,50 U/mL penicillin,and 50μg/mL streptomycin.Cells are grown at 37℃ in an environment of 5% CO2.These cells are seeded on black 96-well assay plates at a density of 15,000 cells/well,and then they are cultured for 24h.   动物实验:   The animals are housed either in pairs or alone under standard conditions at a temperature of 24-26℃ and 50-60% relative humidity using a 12-h light-dark cycle.Diet consisted of standard food pellets,fresh fruit,and Mazuri marmoset jelly.The animals are treated with MPTP in a dose of 2.0mg/kg sc daily for 5 days.Following MPTP treatment the animals are allowed to recover from the acute effects over a period of some 6-8 weeks.During MPTP treatment and throughout the following weeks,the animals are hand-fed with Mazuri marmoset jelly and fresh fruit puree until they are able to maintain themselves.Prior to behavioral testing,from 6-8 weeks to 8 months after exposure to MPTP,all animals show a marked reduction of basal locomotor activity,slower and less coordinated movements,abnormal postures of some parts of the body,and reduced checKing movements and eye blinks.Istradefylline (KW-6002) is suspended in 0.3% Tween-80 and 10% sucrose solution and administered in a final volume of 2.0mL/kg body weight by oral gavage.
保存条件：2-8℃

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