| Identification | Back Directory | [Name]
N-(4-chloropyridin-3-yl)-4-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)Methyl)piperazine-1-carboxaMide | [CAS]
1346528-50-4 | [Synonyms]
CS-2830
JNJ42165279
JNJ-42165279 (JNJ-5279)
JNJ 42165279;JNJ42165279
N-(4-Chloro-3-pyridinyl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-1-piperazinecarboxamide
1-Piperazinecarboxamide, N-(4-chloro-3-pyridinyl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-
N-(4-chloropyridin-3-yl)-4-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)Methyl)piperazine-1-carboxaMide | [Molecular Formula]
C18H17ClF2N4O3 | [MDL Number]
MFCD29047142 | [MOL File]
1346528-50-4.mol | [Molecular Weight]
410.8 |
| Chemical Properties | Back Directory | [Boiling point ]
541.2±50.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
12.91±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
JNJ-42165279 is a potent, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50s = 70 and 313 nM for human and rat forms, respectively). It displays selectivity for FAAH over a panel of other enzymes, receptors, transporters, and ion channels. JNJ-42165279 is active in vivo, blocking FAAH activity in brain and periphery of rats and raising concentrations of anandamide , oleoyl ethanolamide , and palmitoyl ethanolamide . It is also efficacious in the spinal nerve ligation model of neuropathic pain. | [Uses]
JNJ-42165279 is an orally active FAAH inhibitor, with IC50 values of 70 nM for hFAAH and 313 nM for rFAAH. JNJ-42165279 can be used in research related to the field of neuropathic pain[1][2]. | [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]. | [storage]
Store at -20°C | [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. |
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