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PF-06869206  ≥98%

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(≥125mg/ml)
产品描述：基本信息 产品编号： P11298 产品名称： PF-06869206 CAS: 2227425-05-8   储存条件 粉末 -20℃ 四年     分子式： C15H14ClF3N4O2 溶于液体 -80℃ 6个月 分子量： 374.75 -20℃ 1个月 化学名：  (S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile Solubility (25°C)：   体外:   DMSO 75mg/mL (200.13mM) Ethanol 36mg/mL (96.06mM) Water Insoluble 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 2.6684mL 13.3422mL 26.6845mL 5mM 0.5337mL 2.6684mL 5.3369mL 10mM 0.2668mL 1.3342mL 2.6684mL   生物活性 产品描述 一种有效的，具有口服活性的选择性磷酸钠协同转运蛋白NaPi2a(SLC34A1)抑制剂，IC50为380nM。 靶点 IC50:380nM (NaPi2a/SLC34A1)   体外研究 PF-06869206 shows a balance of attributes with 380nM NaPi2a inhibition potency,excellent subtype selectivity,and acceptable aqueous solubility (46μM).PF-06869206 is profiled for potency in the rodent NaPi2a and NaPi2c cell lines.PF06869206 shows comparable submicromolar activity for the human,rat,and mouse NaPi2a isoforms with IC50s of 0.4±0.047μM and 0.54±0.099μM for rat NaPi2a and mouse NaPi2a,respectively. 体内研究 PF-06869206 is evaluated in rodent PK studies to determine suitability for in vivo pharmacology exploration.Results show moderate clearance in both rat and mouse.Oral bioavailability at 5mg/kg is good in rat and moderate in mouse.At higher oral doses of 50mg/kg,supraproportional increases in exposure are observed in both species,suggestive of saturation of clearance.PF-06869206 has moderate terminal elimination half-life (t1/2=1.35h,and 0.75h for Wistar-Han rats (10mg/kg,iv),and C57BL6 mice (1mg/kg,iv)).Furthermore,permeability is good (14×10-6 cm/s),and rat liver microsome (RLM) clearance is low (<14μL/min/mg;HLM=39μL/min/mg).   推荐实验方法(仅供参考) 动物实验:   Rats and Mice Male Wistar-Han rats (n=2) are treated with PF-06869206 (1mg/kg,5mg/kg,and 50mg/kg;2mL/kg for iv or 10mL/kg for po).C57BL6 mice (n=2) are treated with PF-06869206 (1mg/kg,5mg/kg,and 50mg/kg;2mL/kg for iv or 10mL/kg for po).
保存条件：-20℃

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