Biological Activity
Potent and selective reversible MAGL inhibitor (IC50 = 46 nM). Exhibits 35-fold and 150-fold higher selectivity over human FAAH and ABHD6, respectively (IC50 values are 1.79 and 7.24 μM, respectively). Displays affinity for H1 receptors (pA2 = 6.81). Exhibits no activity at cannabinoid receptors at 10 μM.
Technical Data
| M. Wt | 405.88 |
| Formula | C22H20ClN5O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1680193-80-9 |
| PubChem ID | 102596130 |
| InChI Key | GAVZCGTYRWKKDV-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C2C(CCC3=CC=CN=C3/C2=C4CCN(C(N5C=NC=N5)=O)CC4)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.59 | 100 | |
| ethanol | 8.12 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 405.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.46 mL | 12.32 mL | 24.64 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.93 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Patel et al (2015) Loratadine analogues as MAGL inhibitors. Bioorg.Med.Chem.Lett. 25 1436 PMID: 25752982
Keywords: JZP 361, supplier, Potent, selective, reversible, MAGL, inhibitors, inhibits, H1, histamine, receptors, MAGL, MAGL, Tocris Bioscience
