1346528-50-4 Usage
Description
N-(4-chloropyridin-3-yl)-4-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)Methyl)piperazine-1-carboxaMide, also known as JNJ-42165279, is a potent and irreversible inhibitor of fatty acid amide hydrolase (FAAH). It exhibits high selectivity for FAAH over a range of other enzymes, receptors, transporters, and ion channels. JNJ-42165279 is active in vivo, effectively blocking FAAH activity in both the brain and periphery of rats, leading to increased concentrations of anandamide, oleoyl ethanolamide, and palmitoyl ethanolamide.
Uses
Used in Pharmaceutical Industry:
JNJ-42165279 is used as a therapeutic agent for the treatment of neuropathic pain. It has demonstrated efficacy in the spinal nerve ligation model of neuropathic pain, making it a promising candidate for the development of new pain management therapies.
Used in Research Applications:
JNJ-42165279 is utilized as a research tool for studying the role of FAAH and the endocannabinoid system in various physiological and pathological processes. Its selectivity and potency make it a valuable compound for investigating the mechanisms underlying the regulation of endocannabinoid signaling and its potential implications in disease states.
in vitro
jnj-42165279 inhibited recombinant human and rat faah with the ic50s of 70 ± 8 nm and 313 ± 28 nm, respectively [1]. jnj-42165279 (10 μm) exhibited high selectivity against a panel of receptors, enzymes, transporters, and ion-channels. jnj-42165279 (10 μm) showed no inhibitory effects against cyps (1a2, 2c8, 2c9, 2c19, 2d6, 3a4) or herg [1].
in vivo
in the rat spinal nerve ligation (snl or chung) model of neuropathic pain, jnj-42165279 exhibited analgesic properties. jnj-42165279 dose-dependently reversed the robust tactile allodynia. the ed90 was 22 mg/kg, which corresponds to a plasma concentration of 2.5 μm at 30 min [1].
references
[1] keith j m, jones w m, tichenor m, et al. preclinical characterization of the faah inhibitor jnj-42165279[j]. acs medicinal chemistry letters, 2015, 6(12): 1204-1208.
Check Digit Verification of cas no
The CAS Registry Mumber 1346528-50-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,4,6,5,2 and 8 respectively; the second part has 2 digits, 5 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1346528-50:
(9*1)+(8*3)+(7*4)+(6*6)+(5*5)+(4*2)+(3*8)+(2*5)+(1*0)=164
164 % 10 = 4
So 1346528-50-4 is a valid CAS Registry Number.
1346528-50-4Relevant articles and documents
Preclinical Characterization of the FAAH Inhibitor JNJ-42165279
Keith, John M.,Jones, William M.,Tichenor, Mark,Liu, Jing,Seierstad, Mark,Palmer, James A.,Webb, Michael,Karbarz, Mark,Scott, Brian P.,Wilson, Sandy J.,Luo, Lin,Wennerholm, Michelle L.,Chang, Leon,Rizzolio, Michele,Rynberg, Raymond,Chaplan, Sandra R.,Breitenbucher, J. Guy
supporting information, p. 1204 - 1208 (2015/12/23)
The pre-clinical characterization of the aryl piperazinyl urea inhibitor of fatty acid amide hydrolase (FAAH) JNJ-42165279 is described. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channel
