JZP-361
Based on 1 Customer Validation
JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.63%
- CAS 番号: 1680193-80-9
- 分子式: C22H20ClN5O
- 分子量:405.88
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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hMAGL 46 nM (IC50) |
hABHD6 1.79 μM (IC50) |
hFAAH 7.24 μM (IC50) |
H1 Receptor 6.81 (pA2) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
7.24 μM
Compound: JZP-361
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Inhibition of human FAAH expressed in COS7 cell membranes pre-incubated for 10 mins before [3H]-AEA substrate addition by liquid scintillation counting
Inhibition of human FAAH expressed in COS7 cell membranes pre-incubated for 10 mins before [3H]-AEA substrate addition by liquid scintillation counting
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[PMID: 26344596] |
| HEK293 | IC50 |
0.046 μM
Compound: JZP-361
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Inhibition of human MAGL expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method
Inhibition of human MAGL expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method
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[PMID: 26344596] |
| HEK293 | IC50 |
1.78 μM
Compound: JZP-361
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Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method
Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method
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[PMID: 26344596] |
| HEK293 | IC50 |
1.78 μM
Compound: 12a, JZP-361
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Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells
Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells
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[PMID: 25752982] |
JZP-361 has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50 = 7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50 = 1.79 μM)[1].
JZP-361 retains H1 antagonistic affinity (pA2 = 6.81) but did not show cannabinoid receptor activity, when tested at concentrations ≤10 μM[1].
JZP-361 displays favorable interactions within the active site of hMAGL including the important hydrogen-bonding of the carbonyl oxygen to the oxyanion hole[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1680193-80-9
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性状 Solid
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分子量 405.88
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分子式 C22H20ClN5O
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Color White to off-white
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SMILES
O=C(N(CC/1)CCC1=C2C3=C(CCC4=C/2N=CC=C4)C=C(C=C3)Cl)N5N=CN=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (307.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4638 mL | 12.3189 mL | 24.6378 mL | 61.5946 mL |
| 5 mM | 0.4928 mL | 2.4638 mL | 4.9276 mL | 12.3189 mL | |
| 10 mM | 0.2464 mL | 1.2319 mL | 2.4638 mL | 6.1595 mL | |
| 15 mM | 0.1643 mL | 0.8213 mL | 1.6425 mL | 4.1063 mL | |
| 20 mM | 0.1232 mL | 0.6159 mL | 1.2319 mL | 3.0797 mL | |
| 25 mM | 0.0986 mL | 0.4928 mL | 0.9855 mL | 2.4638 mL | |
| 30 mM | 0.0821 mL | 0.4106 mL | 0.8213 mL | 2.0532 mL | |
| 40 mM | 0.0616 mL | 0.3080 mL | 0.6159 mL | 1.5399 mL | |
| 50 mM | 0.0493 mL | 0.2464 mL | 0.4928 mL | 1.2319 mL | |
| 60 mM | 0.0411 mL | 0.2053 mL | 0.4106 mL | 1.0266 mL | |
| 80 mM | 0.0308 mL | 0.1540 mL | 0.3080 mL | 0.7699 mL | |
| 100 mM | 0.0246 mL | 0.1232 mL | 0.2464 mL | 0.6159 mL |
JZP-361 関連分類
HY-121422 関連分類
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