PF 3845

生物活性靶点体外研究体内研究 PF 3845 试剂级价格

PF 3845

CAS号:1196109-52-0
英文名:PF 3845
中文名:PF 3845
CBNumber:CB02518802
分子式:C24H23F3N4O2
分子量:456.46
MOL File:1196109-52-0.mol

PF 3845化学性质

沸点 :623.6±55.0 °C(Predicted)
密度 :1.323±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO: ≥45mg/mL
酸度系数(pKa) :14.14±0.40(Predicted)
形态 :powder
颜色 :white to tan

安全信息

危险品标志 :T
危险类别码 :25
安全说明 :45
危险品运输编号 :UN 2811 6.1 / PGIII
WGK Germany :3

PF 3845性质、用途与生产工艺

生物活性 PF-3845 是一种有效的，选择性的，不可逆和具有口服活性的脂肪酸酰胺水解酶 (FAAH) 抑制剂，Ki 值为 0.23 µM。PF-3845 是将 FAAH 的丝氨酸亲核试剂氨基甲酸酯化的共价抑制剂。PF-3845 可以减少疼痛感，炎症和焦虑/抑郁，而对运动或认知没有实质性影响。
靶点

Ki: 0.23 µM (FAAH)
体外研究

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.

体内研究

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.

用途
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).