| 中文名称: | PF-06869206 | ||||
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| 英文名称: | PF-06869206 | ||||
| 别名: | (S)-3-氯-7-(2-(羟甲基)吗啉)-2-甲基-5-(三氟甲基)-1H-吡咯并[3,2-b]吡啶-6-腈 (S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile | ||||
| CAS No: | 2227425-05-8 | 分子式: | C15H14ClF3N4O2 | 分子量: | 374.75 |
| CAS No: | 2227425-05-8 | ||||
| 分子式: | C15H14ClF3N4O2 | ||||
| 分子量: | 374.75 | ||||
基本信息
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产品编号： |
P11298 |
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产品名称： |
PF-06869206 |
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CAS: |
2227425-05-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
374.75 |
-20℃ |
1个月 |
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化学名： |
(S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile |
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Solubility (25°C)： |
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体外:
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DMSO |
75mg/mL (200.13mM) |
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Ethanol |
36mg/mL (96.06mM) |
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Water |
Insoluble |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.6684mL |
13.3422mL |
26.6845mL |
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5mM |
0.5337mL |
2.6684mL |
5.3369mL |
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10mM |
0.2668mL |
1.3342mL |
2.6684mL |
生物活性
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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。 |
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靶点 |
IC50:380nM (NaPi2a/SLC34A1) |
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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. |
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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)
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动物实验: |
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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). |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
