Description
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.
Product information
CAS Number: 1252765-13-1
Molecular Weight: 489.56
Formula: C26H24FN5O2S
Chemical Name: 1-(4-fluorophenyl)-5-{3-[4-(1,3-thiazole-2-carbonyl)piperazin-1-yl]azetidine-1-carbonyl}-1H-indole
Smiles: O=C(C1C=C2C=CN(C2=CC=1)C1C=CC(F)=CC=1)N1CC(C1)N1CCN(CC1)C(=O)C1=NC=CS1
InChiKey: IVOACCSOISMVBL-UHFFFAOYSA-N
InChi: InChI=1S/C26H24FN5O2S/c27-20-2-4-21(5-3-20)32-9-7-18-15-19(1-6-23(18)32)25(33)31-16-22(17-31)29-10-12-30(13-11-29)26(34)24-28-8-14-35-24/h1-9,14-15,22H,10-13,16-17H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (510.66 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
JNJ-42226314 has IC50s of 1.13 nM, 1.88 nM, 0.67 nM, 0.97 nM for human Hela cells, human PBMC, mouse brain and rat brain, respectively.
In Vivo:
JNJ-42226314 (i.p.; 3 mg/kg and 30 mg/kg; 120 min) dose-dependently elevates hippocampal 2-AG in vivo. 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. JNJ-42226314 (i.p.; 30 mg/kg) is antinociceptive in the rat complete Freund’s adjuvant (CFA) model of inflammatory pain. JNJ-42226314 has t1/2 values of 11.4, 27.6, 27.2 min for MAGL in human, mouse and rat, respectively.
Products are for research use only. Not for human use.
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