PeptideDB

JZL195

CAS: 1210004-12-8 F: C24H23N3O5 W: 433.46

JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibito
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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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.