产品说明书

PF-3845

Print
Chemical Structure| 1196109-52-0 同义名 : -
CAS号 : 1196109-52-0
货号 : A475760
分子式 : C24H23F3N4O2
纯度 : 99%+
分子量 : 456.46
MDL号 : MFCD18382105
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(230.03 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% propylene glycol+5% Tween 80+65% water 15 mg/mL suspension

生物活性
靶点

  • FAAH

    FAAH, Ki:230 nM
描述 FAAH (fatty acid amide hydrolase) is an intracellular membranebound enzyme that principally degrade the endocannabinoid anandamide. It utilizes unusual catalytic triad Ser-Ser-Lys to degrade and inactivate fatty acid amide family of signaling lipids, including the endogenous cannabinoid ligands N-arachidonoylethanolamine (Anandamide, AEA) and 2-arachidonoyl glycerol (2-AG). PF-3845 is an irreversible, highly efficacious and selective FAAH inhibitor with Ki value of 0.23μM. Preincubation with PF-3845 for 1h inhibited hFAAH activity for hydrolysis of its substrate AAMCA. Administration of PF-3845 at dose of 10mg/kg, i.p., for 1-24h inactivated FAAH in the brain of mice as judged by competitive activity-based protein profiling with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845-treated mice (10 mg/kg, i.p.) also showed dramatic elevations in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]. PF-3845-treated animals did not show changes in the levels of 2-AG in brain or liver, suggesting that distinct enzymes regulate this endocannabinoid in vivo. Administration of PF-3845 produced cannabinoid receptor-dependent reductions in inflammatory pain in vivo. Oral administration of PF-3845 at 10 and 30mg/kg caused a dose-dependent inhibition of mechanical allodynia and inhibited pain response in a rat model of inflammatory pain.
作用机制 PF-3845 is a covalent inhibitor that carbamylates FAAH’s serine nucleophile.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL
参考文献

[1]Booker L, Kinsey SG, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol. 2012 Apr;165(8):2485-96.

[2]Booker L, Kinsey SG, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol. 2012 Apr;165(8):2485-96.