PF 3845
中文名称 | PF 3845 |
---|---|
中文同义词 | PF-3845 N-3-吡啶-4-[[3-[[5-(三氟甲基)-2-吡啶]氧基]苯基]甲基]-1-哌啶羧酰胺;N-3-吡啶基-4-[[3-[[5-(三氟甲基)-2-吡啶基]氧基]苯基]甲基]-1-哌啶甲酰胺;N-3-吡啶-4-[[3-[[5-(三氟甲基)-2-吡啶]氧基]苯基]甲基]-1-哌啶羧酰胺;化合物PF-3845;N-(吡啶-3-基)-4-(3-((5-(三氟甲基)吡啶-2-基)氧基)苄基)哌啶-1-酰胺;PF-3845,不可逆FAAH抑制剂 |
英文名称 | PF 3845 |
英文同义词 | PF3845/PF-3845;N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxamide;PF 3845;4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide;N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxamide PF 3845;N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxamide hydrate;PF 3845 hydrate;N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxami |
CAS号 | 1196109-52-0 |
分子式 | C24H23F3N4O2 |
分子量 | 456.46 |
EINECS号 | |
相关类别 | 信号转导通路激酶抑制剂;代谢;小分子抑制剂,天然产物;Pharmaceutical intermediate;Inhibitors;Inhibitor |
Mol文件 | 1196109-52-0.mol |
结构式 |
PF 3845 性质
沸点 | 623.6±55.0 °C(Predicted) |
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密度 | 1.323±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 在DMSO中的溶解度≥45mg/mL |
酸度系数(pKa) | 14.14±0.40(Predicted) |
形态 | 粉末 |
颜色 | 白色至棕褐色 |
Ki: 0.23 µM (FAAH)
PF-3845 (0.5 nM-10 μM; 40 min) inhibits human FAAH-1 (IC
50
=18 nM) in a concentration-dependent manner, and shows negligible activity against FAAH-2 (IC
50
>10 μM) in COS-7 cells.
PF-3845 (0.1-1000 μM; 48 h) significantly decreases the Colo-205 cell viability.
PF-3845 (1-30 mg/kg; p.o.) produces cannabinoid receptor-dependent reductions in inflammatory pain in rat.
PF-3845 (10 mg/kg; a single i.p.) selectively inhibits FAAH in mice for up to 24 hours.
PF-3845 (10 mg/kg; a single i.p.) causes a dramatic and sustained elevation in Anandamide (AEA) in mice.
Animal Model: | Male Sprague-Dawley rats (200g- 250g) are injected CFA |
Dosage: | 1, 3, 10, 30 mg/kg |
Administration: | Oral administration |
Result: | Caused a dose-dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg. |
PF 3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM). Reduces inflammatory pain via a cannabinoid receptor-dependent mechanism. Highly efficacious and selective in vivo. D isplays no activity at FAAH-2 (IC50 >10 μM).
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-14380 | PF-3845 | 1 mg | 278元 | |
2024/01/25 | HY-14380 | PF 3845 PF-3845 | 1196109-52-0 | 5mg | 512元 |