JNJ-42165279
Modify Date: 2025-08-26 09:40:57
JNJ-42165279 structure
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Common Name | JNJ-42165279 | ||
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| CAS Number | 1346528-50-4 | Molecular Weight | 410.802 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 541.2±50.0 °C at 760 mmHg | |
| Molecular Formula | C18H17ClF2N4O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 281.1±30.1 °C | |
Use of JNJ-42165279JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively.IC50 value: 70 ± 8 nM (for hFAAH), 313 ± 28 nM (for rFAAH )Target：FAAHJNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and ion-channels at 10 μM, at which concentration it does not produce >50% inhibition of binding to any of the targets. Fortunately, JNJ-42165279 also does not inhibit CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG when tested at a 10 μM compound concentration. [1]in vivo: JNJ-42165279 exhibits excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting as a low AUC and Cmax; however, sufficiently high exposures were obtainable to support preclinical animal models. In a subsequent higher dose (20 mg/kg) oral PK experiment, compound concentrations were determined both in the plasma and brain of rats. [1] |
| Name | N-(4-Chloro-3-pyridinyl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-1-piperazinecarboxamide |
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| Synonym | More Synonyms |
| Description | JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively.IC50 value: 70 ± 8 nM (for hFAAH), 313 ± 28 nM (for rFAAH )Target：FAAHJNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and ion-channels at 10 μM, at which concentration it does not produce >50% inhibition of binding to any of the targets. Fortunately, JNJ-42165279 also does not inhibit CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG when tested at a 10 μM compound concentration. [1]in vivo: JNJ-42165279 exhibits excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting as a low AUC and Cmax; however, sufficiently high exposures were obtainable to support preclinical animal models. In a subsequent higher dose (20 mg/kg) oral PK experiment, compound concentrations were determined both in the plasma and brain of rats. [1] |
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| Related Catalog | |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 541.2±50.0 °C at 760 mmHg |
| Molecular Formula | C18H17ClF2N4O3 |
| Molecular Weight | 410.802 |
| Flash Point | 281.1±30.1 °C |
| Exact Mass | 410.095734 |
| PSA | 66.93000 |
| LogP | 2.84 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.643 |
| InChIKey | YWGYNGCRVZLMCS-UHFFFAOYSA-N |
| SMILES | O=C(Nc1cnccc1Cl)N1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1 |
| Storage condition | 2-8℃ |
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Name: Diffuse intrinsic pontine glioma (SU-DIPG-XVII) cell line screen of MIPE5.0 library: ...
Source: 15316
Target: N/A
External Id: s-dipg-DIPG17_CTG48h_mipe5_0-1
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Name: qHTS drug screen for cell cycle checkpoint inhibitors in PARPi-resistant BRCA-mutant ...
Source: NCGC
External Id: FGL-PARP_PEO-CTG96h-MIPE5.0-p1
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Name: Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER...
Source: ChEMBL
Target: Severe acute respiratory syndrome coronavirus 2
External Id: CHEMBL4513082
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Name: Human Fatty acid amide hydrolase (Hydrolases)
Source: IUPHAR-DB
Target: Fatty acid amide hydrolase (Hydrolases) [Homo sapiens]
External Id: 1400_Human
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Name: Diffuse intrinsic pontine glioma (SU-DIPG-XXV) cell line screen of MIPE5.0 library: v...
Source: 15316
Target: N/A
External Id: s-dipg-DIPG25-MIPE5.0-CTF48h-p1
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Name: Cellular viability qHTS for adrenocortical cancer (ACC) cell line SW-13
Source: NCGC
Target: N/A
External Id: ACC-ATC-p1-SW13-72hr
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Name: Rat Fatty acid amide hydrolase (Hydrolases)
Source: IUPHAR-DB
Target: Fatty acid amide hydrolase (Hydrolases) [Rattus norvegicus]
External Id: 1400_Rat
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Name: Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac...
Source: ChEMBL
Target: Severe acute respiratory syndrome coronavirus 2
External Id: CHEMBL4303805
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Name: Cellular viability qHTS for adrenocortical cancer (ACC) cell line NCI-H295R
Source: NCGC
Target: N/A
External Id: ACC-ATC-p1-H295R-72hr
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Name: Primary qHTS for inhibitors of nuclear receptor binding SET domain protein 2 (NSD2) i...
Source: NCGC
External Id: NSD2-synergy-p-2C
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| N-(4-chloropyridin-3-yl)-4-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methyl)piperazine-1-carboxamide |
| JNJ-42165279 |
| 4-(2,2-difluorobenzo[1,3]dioxol-5-ylmethyl)piperazine-1-carboxylic acid (4-chloropyridin-3-yl)amide |
| N-(4-Chloro-3-pyridinyl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-1-piperazinecarboxamide |