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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.
分子量 | 405.88 |
公式 | C22H20ClN5O |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.59 | 100 | |
ethanol | 8.12 | 20 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: JZP 361, JZP 361 supplier, Potent, selective, reversible, MAGL, inhibitors, inhibits, H1, histamine, receptors, 5851, Tocris Bioscience
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