| Bioactivity | JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively[1]. | ||||||||||||
| Target | IC50: 2 nM (FAAH), 4 nM (MAGL) | ||||||||||||
| Invitro | JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC50 values of 13 and 19 nM, respectively)[1].JZL195 inhibits rat and human FAAH and MAGL enzymes with IC50 values in the range of ≈10-100 nM based on competitive ABPP assays[1]. | ||||||||||||
| In Vivo | JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay[1]. Animal Model: | ||||||||||||
| Name | JZL195 | ||||||||||||
| CAS | 1210004-12-8 | ||||||||||||
| Formula | C24H23N3O5 | ||||||||||||
| Molar Mass | 433.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Long JZ, 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, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014 Jun;81:224-30. |