PF06869206
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- CAS号:
- 2227425-05-8
- 英文名:
- PF06869206
- 英文别名:
- CS-2762;PF06869206;PF-06869206;PF-06869206; PF 06869206; PF06869206;inhibit,PF-06869206,Na+ channels,Sodium Channel,Na channels,PF 06869206,Inhibitor,PF06869206;(S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile;1H-Pyrrolo[3,2-b]pyridine-6-carbonitrile, 3-chloro-7-[(2S)-2-(hydroxymethyl)-4-morpholinyl]-2-methyl-5-(trifluoromethyl)-
- 中文名:
- PF06869206
- 中文别名:
- 化合物PF-06869206;(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
- CBNumber:
- CB04187431
- 分子式:
- C15H14ClF3N4O2
- 分子量:
- 374.75
- MOL File:
- 2227425-05-8.mol
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PF06869206化学性质
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沸点:
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599.2±50.0 °C(Predicted)
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密度:
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1.57±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMF: 1 mg/mL; DMSO: 1mg/mL; Ethanol: 10mg/mL; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/mL
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形态:
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A crystalline solid
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酸度系数(pKa):
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11.78±0.40(Predicted)
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PF06869206性质、用途与生产工艺
PF-06869206 是一种有效的，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 380 nM。
IC50: 380 nM (NaPi2a/SLC34A1)
PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 μM). PF-06869206 is profiled for potency in the rodent NaPi2a and NaPi2c cell lines. PF-06869206 shows comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms with IC
50
s of 0.4±0.047 μM and 0.54±0.099 μM for rat NaPi2a and mouse NaPi2a, respectively.
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 5 mg/kg is good in rat and moderate in mouse. At higher oral doses of 50 mg/kg, supraproportional increases in exposure are observed in both species, suggestive of saturation of clearance. PF-06869206 has moderate terminal elimination half-life (t
1/2
=1.35 h, and 0.75 h for Wistar-Han rats (10 mg/kg, iv), and C57BL6 mice (1 mg/kg, iv)). Furthermore, permeability is good (14×10
-6
cm/s), and rat liver microsome (RLM) clearance is low (<14 μL/min/mg; HLM=39 μL/min/mg).
PF06869206
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-112065 | PF06869206
PF-06869206 | 2227425-05-8 | 5mg | 920元 |
| 2024/04/30 | HY-112065 | PF06869206
PF-06869206 | 2227425-05-8 | 10mg | 1480元 |
2227425-05-8, PF06869206 相关搜索:
- 药靶配体
- 化合物PF-06869206
- (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
- 2227425-05-8
- inhibit,PF-06869206,Na+ channels,Sodium Channel,Na channels,PF 06869206,Inhibitor,PF06869206
- (S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile
- 1H-Pyrrolo[3,2-b]pyridine-6-carbonitrile, 3-chloro-7-[(2S)-2-(hydroxymethyl)-4-morpholinyl]-2-methyl-5-(trifluoromethyl)-
- PF-06869206; PF 06869206; PF06869206
- CS-2762
- PF-06869206
- PF06869206