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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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J646666-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $350.90 | |
J646666-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $580.90 | |
J646666-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,650.90 | |
J646666-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,450.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | 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 mo |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product 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. In Vitro JNJ-42226314 has IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 t 1/2 values of 11.4, 27.6, 27.2 min for MAGL in human, mouse and rat, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57Bl/6 mice weighing 20-30g and male Sprague-Dawley rats weighing 300-400 g Dosage: 3 mg/kg and 30 mg/kg Administration: i.p.; 120 min Result: Dose-dependently elevated hippocampal 2-AG in vivo. Form:Solid |
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IUPAC Name | [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(1,3-thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone |
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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 |
InChi Key | IVOACCSOISMVBL-UHFFFAOYSA-N |
Canonical SMILES | C1CN(CCN1C2CN(C2)C(=O)C3=CC4=C(C=C3)N(C=C4)C5=CC=C(C=C5)F)C(=O)C6=NC=CS6 |
Isomeric SMILES | C1CN(CCN1C2CN(C2)C(=O)C3=CC4=C(C=C3)N(C=C4)C5=CC=C(C=C5)F)C(=O)C6=NC=CS6 |
PubChem CID | 59625954 |
Molecular Weight | 489.56 |
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Solubility | DMSO : 250 mg/mL (510.66 mM; Need ultrasonic) |
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