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Submit ReviewKML 29 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor. Exhibits potent inhibition of human, mouse and rat MAGL (IC50 values are 5.9, 15 and 43 nM, respectively). Exhibits no detectable inhibition of FAAH (IC50 > 50000 nM). Potently and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50 = 2.5 nM and >50 μM for 2-AG and AEA respectively).
Sold under license from The Scripps Research Institute
KML 29 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 549.42 |
公式 | C24H21F6NO7 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1380424-42-9 |
PubChem ID | 71656212 |
InChI Key | SXHQLPHDBLTFPM-UHFFFAOYSA-N |
Smiles | O=C(OC(C(F)(F)F)C(F)(F)F)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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 54.94 | 100 |
以下数据基于产品分子量 549.42。 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 | 1.82 mL | 9.1 mL | 18.2 mL |
5 mM | 0.36 mL | 1.82 mL | 3.64 mL |
10 mM | 0.18 mL | 0.91 mL | 1.82 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
参考文献是支持产品生物活性的出版物。
Ueda et al (2012) Discrimination between two endocannabinoids. Chem.Biol. 19 545 PMID: 22633404
Chang et al (2012) Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem.Biol. 19 579 PMID: 22542104
If you know of a relevant reference for KML 29, please let us know.
关键词: KML 29, KML 29 supplier, KML29, MAGL, inhibitor, MAG, lipase, monoacylglycerol, inhibitors, MGL, endocannabinoids, 2, AG, arachidonoylethanolamide, anandamide, inhibits, 4872, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 KML 29 的部分引用包括:
Morena et al (2016) Emotional arousal state influences the ability of amygdalar endocannabinoid signaling to modulate anxiety. Neuropharmacology 111 59 PMID: 27553121
Margaret M et al (2019) Microglial Phagocytosis of Newborn Cells Is Induced by Endocannabinoids and Sculpts Sex Differences in Juvenile Rat Social Play. Neuron 102 435-449.e6 PMID: 30827729
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