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KML29

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Chemical Structure| 1380424-42-9 同义名 : -
CAS号 : 1380424-42-9
货号 : A215224
分子式 : C24H21F6NO7
纯度 : 98%
分子量 : 549.417
MDL号 : MFCD22987957
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(91.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 KML29, known for its high selectivity, oral activity, and irreversible inhibition of MAGL, showcases IC50 values of 15 nM, 43 nM, and 5.9 nM for mouse, rat, and human MAGL respectively. This inhibitor has minimal cross-reactivity towards other central and peripheral serine hydrolases, including an absence of detectable activity against FAAH[1].[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.82mL

0.36mL

0.18mL

9.10mL

1.82mL

0.91mL

18.20mL

3.64mL

1.82mL
参考文献

[1]Natsuo Ueda, et al. Discrimination between two endocannabinoids. Chem Biol. 2012 May 25;19(5):545-7.

[2]Jae Won Chang, et al. Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem Biol. 2012 May 25;19(5):579-88.

[3]B M Ignatowska-Jankowska, et al. In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects. Br J Pharmacol. 2014 Mar;171(6):1392-407.