Free shipping on all orders over $ 500

PF-3845

Cat. No. M3525
PF-3845 Structure
Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 380 In stock
200mg USD 1020 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PF-3845 is a potent, selective, and irreversible fatty acid amide hydrolase (FAAH) inhibitor with a Ki of 0.23 μM. Fatty acid amide hydrolase (FAAH) is an enzyme that catalyzes N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). Mechanistic and structural studies demonstrated that PF-3845 acts as a covalent inhibitor and carbamylates the active site serine241 of FAAH. PF-3845 covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment. Initial experiments indicated that PF-3845 is 10 to 20 times more potent than other FAAH inhibitors and has superior pharmacokinetic properties. PF-3845 significantly and persistently blockes inflammatory pain in rats through a cannabinoid receptor-dependent mechanism. In animal studies, PF-3845 elevated brain anandamide levels for up to 24 hours and produced a marked cannabinoid receptor-dependent reduction in inflammatory pain.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male C57BL/6 mice
Formulation PF-3845 is dissolved at 1 mg/ml by sonication and vortexing directly into a solution of 18:1:1 v/v/v saline:emulphor:ethanol.
Dosages 10 mg/kg or 1-30 mg/kg
Administration Administered via i.p. 1 hour before sacrificed by CO2 or oral administration.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 456.46
Formula C24H23F3N4O2
CAS Number 1196109-52-0
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
Related FAAH Products
FAAH-IN-2

FAAH-IN-2 is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.

URB597

URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.

JNJ-1661010

JNJ-1661010 is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-3845 supplier, FAAH, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.