Molecular Formula | C24H23N3O5 |
Molar Mass | 433.46 |
Density | 1.303±0.06 g/cm3(Predicted) |
Boling Point | 581.8±50.0 °C(Predicted) |
Solubility | DMSO : 50 mg/mL (115.35 mM; Need ultrasonic) |
Appearance | powder |
Color | white to beige |
pKa | 6.13±0.10(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Use | JZL195 is an effectively selected dual inhibitor of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) with IC50s of 2 and 4 nM, respectively. |
In vitro study | JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC 50 values of 13 and 19 nM, respectively). JZL195 inhibits rat and human FAAH and MAGL enzymes with IC 50 values in the range of ≈10-100 nM based on competitive ABPP assays. |
In vivo study | JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay. Animal Model: Male C57BL/6J mice Dosage: 20 mg/kg Administration: Intraperitoneal injection Result: Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone. |
Hazard Symbols | N - Dangerous for the environment |
Risk Codes | 50 - Very Toxic to aquatic organisms |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.307 ml | 11.535 ml | 23.07 ml |
5 mM | 0.461 ml | 2.307 ml | 4.614 ml |
10 mM | 0.231 ml | 1.154 ml | 2.307 ml |
5 mM | 0.046 ml | 0.231 ml | 0.461 ml |
biological activity | JZL195 is a potent FAAH and MAGL inhibitor with IC50 of 2 nM and 4 nM, respectively. |
Target | TargetValue FAAH () 2 nM MAGL () 4 nM |
Target | Value |
FAAH () | 2 nM |
MAGL () | 4 nM |
In vitro studies | JZL195 products near-complete block of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC 50 values 13 and 19 nM, review). JZL195 inhibitors rat and human FAAH and MAGL enzymes with IC 50 values in the range of ≈ 10-100 nM based on competitive ABPP asays. |
in vivo studies | JZL195 (20 mg/kg; I. p.) produces an antinociceptive response in the tail immersion assay. Animal Model: Male C57BL/6J mice Dosage: 20 mg/kg: produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone. |
Animal Model: | Male C57BL/6J mice |
Dosage: | 20 mg/kg |
Administration: | Intraperitoneal injection |
Result: | Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone. |