898235-65-9 Usage
Description
PF-622 is a potent and selective irreversible fatty acid amide hydrolase (FAAH) inhibitor. It covalently modifies the active site-serine with an IC50 of 33 nM and is completely selective for FAAH relative to other mammalian serine hydrolases. PF-622 is also cell permeable, making it a promising candidate for various applications.
Uses
Used in Pharmaceutical Industry:
PF-622 is used as a therapeutic agent for the treatment of pain and inflammation. Its ability to irreversibly inhibit FAAH, an enzyme responsible for the degradation of endocannabinoids, leads to increased levels of endocannabinoids such as anandamide. This results in enhanced endocannabinoid signaling, which has been implicated in the modulation of pain and inflammation.
Used in Neurological Disorders Research:
PF-622 is used as a research tool for studying the role of the endocannabinoid system in neurological disorders. Its selectivity and potency in inhibiting FAAH make it an ideal compound for investigating the therapeutic potential of modulating endocannabinoid signaling in conditions such as multiple sclerosis, Alzheimer's disease, and Parkinson's disease.
Used in Drug Development:
PF-622 is used as a lead compound in the development of new drugs targeting the endocannabinoid system. Its unique mechanism of action and selectivity for FAAH make it a valuable starting point for designing and optimizing novel therapeutic agents with improved efficacy, safety, and pharmacokinetic properties.
in vitro
pf-622 inhibited the activity of faah in a time-dependent manner with the ic50 values of 0.99 and 0.033 μm in human recombinant faah for 5 and 60 minutes, respectively [1]. in various human and murine tissue proteome samples, pf-622 showed highly selectivity for faah in relative to other serine hydrolases, showing no discernable off-site activity up to 500 μm [1]. pf-622 at 1 μm decreased il-2 production in both healthy subjects and in hcv patients [2].
References
1) Ahn et al. (2007), Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity; Biochemistry, 46 13019
Check Digit Verification of cas no
The CAS Registry Mumber 898235-65-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,9,8,2,3 and 5 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 898235-65:
(8*8)+(7*9)+(6*8)+(5*2)+(4*3)+(3*5)+(2*6)+(1*5)=229
229 % 10 = 9
So 898235-65-9 is a valid CAS Registry Number.
898235-65-9Relevant articles and documents
Preparation of tritium-labeled PF-622, a novel fatty acid amide hydrolase inhibitor
Zhang, Yinsheng
, p. 608 - 615 (2017)
To make a detailed characterization of the mechanism of inhibition and selectivity of a novel fatty acid amide hydrolase inhibitor PF-622, 3 tritium isotopomers were prepared. [3H]PF-622a labeled at the piperazine ring B and [3H]PF-622b labeled at both the ring B and phenyl ring A were synthesized via catalytic H(hydrogen)-T(tritium) exchange, utilizing 1 equiv and excess of Crabtree's catalyst, respectively. The preparation of [3H]PF-622c labeled only at the phenyl ring A was achieved via tritiodebromination of the bromide precursor, using Pd(PPh3)4 as a catalyst. The observations from these tritiation reactions might open a new perspective in the labeling for the targets having a similar moiety.
