1196109-52-0
中文名稱
PF 3845
英文名稱
PF 3845
CAS
1196109-52-0
分子式
C24H23F3N4O2
分子量
456.46
MOL 文件
1196109-52-0.mol
更新日期
2024/06/03 14:41:43
1196109-52-0 結(jié)構(gòu)式
基本信息
中文別名
化合物PF-3845N-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
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
英文別名
CS-124PF 3845
PF3845/PF-3845
PF 3845 hydrate
PF 3845 USP/EP/BP
PF-3845
PF 3845
PF3845
4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide
N-(Pyridin-3-yl)-4-(3-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzyl)piperidine-1-carboxamide
N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxami
N-pyridin-3-yl-4-[[3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl]methyl]piperidine-1-carboxamide
所屬類別
生物化工：FAAH 抑制劑物理化學(xué)性質(zhì)
沸點623.6±55.0 °C(Predicted)
密度1.323±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度在DMSO中的溶解度≥45mg/mL
酸度系數(shù)(pKa)14.14±0.40(Predicted)
形態(tài)粉末
顏色白色至棕褐色
應(yīng)用領(lǐng)域
用途1
PF 3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 渭M). Reduces inflammatory pain via a cannabinoid receptor-dependent mechanism. Highly efficacious and selective in vivo. D
isplays no activity at FAAH-2 (IC50 >10 渭M).常見問題列表
生物活性
PF-3845 是一種有效的，選擇性的，不可逆和具有口服活性的脂肪酸酰胺水解酶 (FAAH) 抑制劑，Ki 值為 0.23 μM。PF-3845 是將 FAAH 的絲氨酸親核試劑氨基甲酸酯化的共價抑制劑。PF-3845 可以減少疼痛感，炎癥和焦慮/抑郁，而對運動或認(rèn)知沒有實質(zhì)性影響。靶點
Ki: 0.23 μM (FAAH)
體外研究
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.
體內(nèi)研究
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. |