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Toreforant  ≥98%

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包装规格：1mg 5mg 25mg in glass bottle
产品描述：基本信息 产品编号： T11452 产品名称： Toreforant CAS: 952494-46-1   储存条件 粉末 -20℃ 四年 分子式： C23H32N6 溶于液体 -80℃ 二年 分子量 392.54     化学名：  5-(4,6-dimethyl-1H-benzimidazol-2-yl)-4-methyl-N-[3-(1-methylpiperidin-4-yl)propyl]pyrimidin-2-amine 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 一种有效的、选择性的组胺 H4 (H4R) 受体拮抗剂，人类中的 Ki 值为 8.4nM。 靶点 H4 receptor 8.4±2.2nM (IC50)   体外研究 In human polymorphonuclear leukocytes,Toreforant inhibits the histamine-induced shape change of human eosinophils and produces a rightward shift in the histamine dose response curves indicating that it is acting as an antagonist of the human H4R in these primary cells.This is not an equilibrium measurement and therefore the calculation of a pA2 is complicated.The pA2 can be estimated using the shift seen the lowest concentration of antagonist.This yields a pA2 of around 7.5 consistent with the results in the transfected system.This assay can also be performed in whole blood and,as for the purified cells,Toreforant is able to inhibit the actions of histamine.The IC50 values are 296nM and 780nM when 100nM and 300nM histamine are used,respectively. 体内研究 The animals treated with 100mg/kg toreforant have reduced disease severity scores.The reduction in scores is similar to JNJ 28307474.A model of histamine-induced scratching in CD-1 mice (n=5 per group) is used to judge the anti-pruritic effects of Toreforant.Unlike other H4R antagonists,Toreforant is not efficacious in reducing histamine-mediated pruritus.After oral administration to rats,Toreforant-derived radioactivity is widely distributed into tissues;however,it is not quantifiable in cerebellum,cerebrum,medulla, and spinal cord in either Long Evans or Sprague Dawley rats,suggesting that drug-derived radioactivity does not cross the blood-brain barrier.Neuropathic pain models in rats are conducted with Toreforant and an H4R antagonist that does cross the blood-brain barrier,JNJ 39758979.In a rat spinal nerve ligation model JNJ 39758979 was able to significantly attenuate the mechanical allodynia induced in the model,however Toreforant has no activity.   推荐实验方法(仅供参考) 动物实验:   Mice The ovalbumin mouse asthma model and the collageninduced arthritis model are conducted.Toreforant is dosed orally in 20% hydroxypropyl-β-cyclodextrin.In the collagen-induced arthritis model Toreforant is given orally twice a day starting with the first signs of disease onset around Day 30 and continued for 14 days.CD-1 mice (5 per group) are dosed with vehicle (20% hydroxypropyl-β-cyclodextrin),Toreforant or JNJ 28307474,as a positive control,at 50mg/kg orally,60 mins prior to the intra-dermal injection of histamine.Bouts of scratching are recorded over a 20 minute period.In a subsequent experiment mice are orally dosed with Toreforant (100mg/kg) at 24,8,4 and 1h prior to intra-dermal injection of histamine and similarly monitored.The area at the back of the neck of mice is shaved 24 hours prior to an intra-dermal injection of 20μL of 100μg compound 48/80.Both knockout and wild-type mice (five mice per group) are dosed with vehicle,Toreforant (50mg/kg) or JNJ 28307474 (50mg/kg),orally, 60 mins prior to the intradermal injection.Bouts of scratching are recorded over a 20 minute period.Terminal (t=80 min) plasma and brain samples are analyzed for drug concentration.Male SpragueDawley rats are deeply anesthetized with isoflurane/oxygen inhalational anesthesia .
保存条件：-20℃

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