Loading... Please wait...

Our Newsletter


PF-3845 | FAAH inhibitor

  • PF-3845.jpg
  • PF-3845, 400x400px, png
Price:
$89.00
Catalog #:
C7384-5
Quantity:


Product Description

PF-3845 is an orally-available, covalent and irreversible inhibitor of fatty acid amide hydrolase (FAAH) for the treatment of inflammation and pain, with an IC50 of 7.2 nM. [1] Mechanistic studies show that PF-3845 is a time-dependent inhibitor that carbamylates FAAH's catalytic serine nucleophile and raises anandamide levels in the brain for up to 24h. [2, 3]

Oral administration of PF-3845 produces antinociceptive effects in both inflammatory and noninflammatory pain models in rats with an MED 0.1 mg/kg. [2] Furthermore, oral administration of PF-3845 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat inflammatory pain model. [1]

Regarding the encannabinoid system, PF-3845 has been shown to be an effective treatment (i.p.) for the blockade of neuronal FAAH to reverse allodynia through the activation of both cannabinoid receptors, without the psychomimetic side effects associated with THC. [4]


Technical information:

Chemical Formula:   C24H23F3N4O2
CAS #:   1196109-52-0
Molecular Weight:   456.46
Purity:   >98%
Appearance:   White
Chemical Name:   4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   PF-3845, PF 3845, PF3845

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Johnson et al., Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med. Chem. Lett. 2011, 2, 91-96. Pubmed ID: 21666860
2. Ahn et al., Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J. Pharmcol. Exp. Ther. 2011, 338 (1), 114-124. Pubmed ID: 21505060
3. Ahn et al., Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem. Biol. 2009, 16(4), 411-420. Pubmed ID: 19389627
4. Booker 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. Pubmed ID: 21505060

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the PF-3845 | FAAH inhibitor to your wish list.

You Recently Viewed...