JNJ-42226314
- Product Name
- JNJ-42226314
- CAS No.
- 1252765-13-1
- Chemical Name
- JNJ-42226314
- Synonyms
- Compound 6g;JNJ-42226314;JNJ42226314,JNJ 42226314;JNJ-42226314, 10 mM in DMSO;1-(4-Fluorophenyl)-5-indolyl][3-[4-(thiazole-2-carbonyl)-1-piperazinyl]-1-azetidinyl]methanone;1-(4-fluorophenyl)-5-{3-[4-(1,3-thiazole-2-carbonyl)piperazin-1-yl]azetidine-1-carbonyl}-1H-indole;(1-(4-Fluorophenyl)-1H-indol-5-yl)(3-(4-(thiazole-2-carbonyl)piperazin-1-yl)azetidin-1-yl)methanone;Methanone, [4-[1-[[1-(4-fluorophenyl)-1H-indol-5-yl]carbonyl]-3-azetidinyl]-1-piperazinyl]-2-thiazolyl-
- CBNumber
- CB18054439
- Molecular Formula
- C26H24FN5O2S
- Formula Weight
- 489.56
- MOL File
- 1252765-13-1.mol
JNJ-42226314 Property
- Boiling point:
- 624.9±65.0 °C(Predicted)
- Density
- 1.44±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: 2mg/mL, clear
- form
- Solid
- pka
- 5.68±0.70(Predicted)
- color
- White to off-white
- InChIKey
- IVOACCSOISMVBL-UHFFFAOYSA-N
- SMILES
- C(N1CCN(C2CN(C(C3C=CC4=C(C=3)C=CN4C3=CC=C(F)C=C3)=O)C2)CC1)(C1=NC=CS1)=O
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
N-Bromosuccinimide Price
- Product number
- 41115
- Product name
- JNJ-42226314
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2026/04/30
- Product number
- 41115
- Product name
- JNJ-42226314
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $145
- Updated
- 2026/04/30
- Product number
- 41115
- Product name
- JNJ-42226314
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $240
- Updated
- 2026/04/30
- Product number
- 41115
- Product name
- JNJ-42226314
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $479
- Updated
- 2026/04/30
- Product number
- CS-0112147
- Product name
- JNJ-42226314
- Purity
- 99.59%
- Packaging
- 10mg
- Price
- $580
- Updated
- 2021/12/16
JNJ-42226314 Chemical Properties,Usage,Production
Uses
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain[1].
Biological Activity
Brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL).
JNJ-42226314 is a brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL)(IC50 = 1.1) th at exhibits antinociceptive efficacy in the r at models neuropathic and inflammatory pain. JNJ-42226314 elevates hippocampal 2-arachidonoylglycerol (2-AG) levels and prolongs wakefulness in rats.
in vivo
JNJ-42226314 (i.p.; 3 mg/kg and 30 mg/kg; 120 min) dose-dependently elevates hippocampal 2-AG in vivo[1].
JNJ-42226314 (i.p.; 30 mg/kg)significantly increases total wake time for up to 8 hours afterward, whereas total wake time was only elevated for 2 hr following a 3 mg/kg dose[1].
JNJ-42226314 (i.p.; 30 mg/kg) is antinociceptive in the rat complete Freund’s adjuvant (CFA) model of inflammatory pain[1].
JNJ-42226314 has t1/2 values of 11.4, 27.6, 27.2 min for MAGL in human, mouse and rat, respectively[1].
| Animal Model: | Male C57Bl/6 mice weighing 20-30g and male Sprague-Dawley rats weighing 300-400 g[1] |
| Dosage: | 3 mg/kg and 30 mg/kg |
| Administration: | i.p.; 120 min |
| Result: | Dose-dependently elevated hippocampal 2-AG in vivo. |
References
[1] Wyatt RM, et al.Pharmacologic characterization of JNJ-42226314, [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a reversible, selective and potent monoacylglycerol lipase inhibitor.J Pharmacol Exp Ther. 2019 Dec 9. DOI:10.1124/jpet.119.262139
JNJ-42226314 Preparation Products And Raw materials
Raw materials
Preparation Products
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