JZL195

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Chemical Structure| 1210004-12-8 同义名 : -
CAS号 : 1210004-12-8
货号 : A905609
分子式 : C24H23N3O5
纯度 : 98%
分子量 : 433.457
MDL号 : MFCD18382122
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(115.35 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 JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 values of 2nM and 4nM, respectively. It exhibited broad activity in the tetrad test for CB1 agonism, causing analgesia, hypomotilty, and catalepsy. Male C57BL/6 mice administered JZL195 at doses ranging in 3–20mg/kg, i.p., for 4h showed dose-dependent reductions in brain FAAH, MAGL, and ABHD6 activities as judged by gel-based ABPP that correlated with near-complete inhibition of both AEA and 2-AG hydrolysis[6]. JZL195 reduced inflammation induced allodynia, mechanical allodynia and thermal hyperalgesia, as well as produced catalepsy and sedation in a dose dependent manner. It displays greater efficacy than FAAH or MAGL specific inhibitors[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL
参考文献

[1]Long JZ, Nomura DK, et al. Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20270-5.

[2]Anderson WB, Gould MJ, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014 Jun;81:224-30.

[3]Bedse G, Bluett RJ, et al. Therapeutic endocannabinoid augmentation for mood and anxiety disorders: comparative profiling of FAAH, MAGL and dual inhibitors. Transl Psychiatry. 2018 Apr 26;8(1):92.

[4]Hruba L, Seillier A, et al. Simultaneous inhibition of fatty acid amide hydrolase and monoacylglycerol lipase shares discriminative stimulus effects with Δ9-tetrahydrocannabinol in mice. J Pharmacol Exp Ther. 2015 May;353(2):261-8.

[5]Adamson Barnes NS, Mitchell VA, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine neuropathic pain model. Br J Pharmacol. 2016 Jan;173(1):77-87.

[6]Long JZ, Nomura DK, Vann RE, Walentiny DM, Booker L, Jin X, Burston JJ, Sim-Selley LJ, Lichtman AH, Wiley JL, Cravatt BF. Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20270-5. doi: 10.1073/pnas.0909411106. Epub 2009 Nov 16. PMID: 19918051; PMCID: PMC2787168.

[7]Anderson WB, Gould MJ, Torres RD, Mitchell VA, Vaughan CW. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014 Jun;81:224-30. doi: 10.1016/j.neuropharm.2013.12.018. Epub 2013 Dec 30. PMID: 24384256.