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Submit ReviewJZP 361 is a 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.
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)CC\4)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 40.59 | 100 | |
ethanol | 8.12 | 20 |
The following data is based on the product molecular weight 405.88. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
Patel et al (2015) Loratadine analogues as MAGL inhibitors. Bioorg.Med.Chem.Lett. 25 1436 PMID: 25752982
If you know of a relevant reference for JZP 361, please let us know.
Keywords: JZP 361, JZP 361 supplier, Potent, selective, reversible, MAGL, inhibitors, inhibits, H1, histamine, receptors, 5851, Tocris Bioscience
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