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Submit ReviewJZL 184
说明： Potent MAGL inhibitor
化学名： 4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 4-nitrophenyl ester
纯度： ≥98% (HPLC)
生物活性 for JZL 184
JZL 184 is a potent and selective MAGL inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nM). Potentiates depolarization-induced suppression of excitability in cerebellar Purkinje neurons. Exhibits >300-fold selectivity for MAGL over FAAH in vitro. Attenuates nociception in neuropathic and inflammatory pain models. Also reduces free fatty acid levels in primary tumors.
许可信息
Sold under license from The Scripps Research Institute.
化合物库 for JZL 184
JZL 184 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for JZL 184
| 分子量 | 520.49 |
| 公式 | C27H24N2O9 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1101854-58-3 |
| PubChem ID | 25021165 |
| InChI Key | SEGYOKHGGFKMCX-UHFFFAOYSA-N |
| Smiles | O=C(OC6=CC=C([N+]([O-])=O)C=C6)N(CC5)CCC5C(C2=CC=C(OCO3)C3=C2)(O)C1=CC(OCO4)=C4C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for JZL 184
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 52.05 | 100 |
制备储备液 for JZL 184
以下数据基于产品分子量 520.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.92 mL | 9.61 mL | 19.21 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.84 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.92 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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产品说明书 for JZL 184
参考文献 for JZL 184
参考文献是支持产品生物活性的出版物。
Long et al (2009) Selective blockade of 2-arachidonylglycerol hydrolysis produces cannabinoid behavioral effects. Nat.Chem.Biol. 5 37 PMID: 19029917
Pan et al (2009) Blockade of 2-arachidonylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) enhances retrograde endocannabinoid signaling. J.Pharm.Exp.Ther. 331 591 PMID: 19666749
Kinsey et al (2013) Repeated low-dose administration of the monoacylglycerol lipase inhibitor JZL184 retains cannabinoid receptor type 1-mediated antinociceptive and gastroprotective effects. J.Pharmacol.Exp.Ther. 345 492 PMID: 23412396
Zhang et al (2012) Dysregulated lipid metabolism in cancer. World J.Biol.Chem. 3 167 PMID: 22937213
If you know of a relevant reference for JZL 184, please let us know.
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关键词: JZL 184, JZL 184 supplier, JZL184, MAGL, inhibitor, MAG, lipase, monoacylglycerol, inhibitors, inhibits, MGL, 3836, Tocris Bioscience
12 篇 JZL 184 的引用文献
引用文献是使用了 Tocris 产品的出版物。 JZL 184 的部分引用包括：
Miriam et al (2020) 2-arachidonoylglycerol reduces chondroitin sulphate proteoglycan production by astrocytes and enhances oligodendrocyte differentiation under inhibitory conditions. Glia 68 1255-1273 PMID: 31894889
Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Stem Cells Dev 9 457 PMID: 26648844
Sardinha et al (2014) Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis. Front Cell Neurosci 2014 978678 PMID: 24803745
Argueta et al (2019) Cannabinoid CB1 Receptors Inhibit Gut-Brain Satiation Signaling in Diet-Induced Obesity. Front Physiol 10 704 PMID: 31281260
Iryna M et al (2021) Increased 2-arachidonoyl-sn-glycerol levels normalize cortical responses to sound and improve behaviors in Fmr1 KO mice. J Neurodev Disord 13 47 PMID: 34645383
Gary et al (2021) Rapid Aging in the Perforant Path Projections to the Rodent Dentate Gyrus. J Neurosci 41 2301-2312 PMID: 33514675
Hu et al (2019) Endocannabinoid Signaling Mediates Local Dendritic Coordination between Excitatory and Inhibitory Synapses. Cell Rep 27 666 PMID: 30995465
Bashashati et al (2015) Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation. Br J Pharmacol 172 3099 PMID: 25684407
Praveen et al (2022) The Endocannabinoid Analgesic Entourage Effect: Investigations in Cultured DRG Neurons. J Pain Res 15 3493-3507 PMID: 36394060
Giulio G et al (2022) Identification of an endocannabinoid gut-brain vagal mechanism controlling food reward and energy homeostasis. Mol Psychiatry 27 2340-2354 PMID: 35075269
Valdeolivas et al (2013) The inhibition of 2-arachidonoyl-glycerol (2-AG) biosynthesis, rather than enhancing striatal damage, protects striatal neurons from malonate-induced death: a potential role of cyclooxygenase-2-dependent metabolism of 2-AG. Cell Death Dis 4 e862 PMID: 24136226
Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release. J Biol Chem 288 32685 PMID: 24089517
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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