898235-65-9 Usage
Description
PF-622 (898235-65-9) is a potent and selective irreversible FAAH inhibitor. Covalently modifies active site-serine (IC50=33 nM). Completely selective for FAAH relative to other mammalian serine hydrolases. Cell permeable
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.
