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Formula | C27H24N2O9 |
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Molecular Weight | 520.49 | CAS No. | 1101854-58-3 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (192.12 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | JZL 184 is the first selective inhibitor of monoacylglycerol lipase (MAGL) with IC50 of 8 nM. | ||
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In vitro | JZL184 is a useful tool for studying the effects of endogenous 2-AG signaling. JZL184 displays time-dependent inhibition of MAGL and exhibits >300-fold selectivity for MAGL over FAAH in vitro. JZL184 does not interact with CB1 or CB2 receptors and does not inhibit the 2-AG biosynthetic enzymes diacylglycerol lipase-αand diacylglycerol lipase-β, or the arachidonic acid–mobilizing enzyme cytosolic phospholipase A2 group IVA. [1] | ||
In vivo | JZL184 produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in eight-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL184-treated mice showed a wide array of CB1-dependent behavioral effects, including analgesia, hypomotility and hypothermia, that suggest a broad role for 2-AG–mediated endocannabinoid signaling throughout the mammalian nervous system. [1] |
Kinase Assay:[1] |
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Cell Assay:[2] |
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Animal Study:[1] |
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Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] | PubMed: 35332332 |
Identification of bioactive natural products using yeast:Application to monoacylglycerol lipase inhibitor extraction from Corydalis Rhizoma [ Biomed Pharmacother, 2022, 149:112798] | PubMed: 35286964 |
Myeloid But Not Endothelial Expression of the CB2 Receptor Promotes Atherogenesis in the Context of Elevated Levels of the Endocannabinoid 2-Arachidonoylglycerol [ J Cardiovasc Transl Res, 2022, 10.1007/s12265-022-10323-z] | PubMed: 36178662 |
Alterations of the endocannabinoid system and its therapeutic potential in autism spectrum disorder [ Open Biol, 2021, 11(2):200306] | PubMed: 33529552 |
Enhanced monoacylglycerol lipolysis by ABHD6 promotes NSCLC pathogenesis. [ EBioMedicine, 2020, 53:102696] | PubMed: 32143183 |
Chlamydia pneumoniae infection-induced endoplasmic reticulum stress causes fatty acid-binding protein 4 secretion in murine adipocytes. [ J Biol Chem, 2020, 295(9):2713-2723] | PubMed: 31992597 |
Lipid accumulation and oxidation in glioblastoma multiforme [ Sci Rep, 2019, 9(1):19593] | PubMed: 31863022 |
p21-activated kinase 1 restricts tonic endocannabinoid signaling in the hippocampus [ Elife, 2016, 5e14653] | PubMed: 27296803 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.