PF-3845_product_DataBase

Bioactivity

PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 µM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition[1][3].

Target

Ki: 0.23 µM (FAAH)

Invitro

PF-3845 (0.5 nM-10 μM; 40 min) inhibits human FAAH-1 (IC50=18 nM) in a concentration-dependent manner, and shows negligible activity against FAAH-2 (IC50>10 μM) in COS-7 cells[1].PF-3845 (0.1-1000 μM; 48 h) significantly decreases the Colo-205 cell viability[2].

In Vivo

PF-3845 (1-30 mg/kg; p.o.) produces cannabinoid receptor-dependent reductions in inflammatory pain in rat[1].PF-3845 (10 mg/kg; a single i.p.) selectively inhibits FAAH in mice for up to 24 hours[1].PF-3845 (10 mg/kg; a single i.p.) causes a dramatic and sustained elevation in Anandamide (AEA) in mice[1]. Animal Model:

Name

PF-3845

CAS

1196109-52-0

Formula

C24H23F3N4O2

Molar Mass

456.46

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Ahn K, et al. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol. 2009 Apr 24;16(4):411-20. [2]. Wasilewski A, et, al. Fatty acid amide hydrolase (FAAH) inhibitor PF-3845 reduces viability, migration and invasiveness of human colon adenocarcinoma Colo-205 cell line: an in vitro study. Acta Biochim Pol. 2017;64(3):519-525. [3]. Booker L, 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, 165(8), 2485-2496.

PeptideDB

PF-3845

CAS: 1196109-52-0 F: C24H23F3N4O2 W: 456.46