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JNJ-42226314

Cat. No. M13413
JNJ-42226314  Structure
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Biological Activity

JNJ-42226314 is a competitive, highly selective and reversible inhibitor of non-covalent monoacylglycerol lipase (MAGL). The IC50s of JNJ-42226314 against human Hela cells, human PBMC, mouse brain and rat brain were 1.13 nM, 1.88 nM, 0.67 nM and 0.97 nM, respectively.

Chemical Information
Molecular Weight 489.56
Formula C26H24FN5O2S
CAS Number 1252765-13-1
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ryan M Wyatt, et al. J Pharmacol Exp Ther. 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

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  Catalog
Abmole Inhibitor Catalog




Keywords: JNJ-42226314 supplier, MAGL, inhibitors, activators


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