SAR629
Based on 1 Customer Validation
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation.
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- Reinheit: 99.93%
- CAS. Nr.: 1221418-42-3
- Formel: C20H19F2N5O
- Molecular Weight:383.39
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
282 nM
Compound: SAR629
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Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
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[PMID: 25282655] |
| HEK293 | IC50 |
0.9 nM
Compound: SAR629
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Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
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[PMID: 25282655] |
SAR629 is a potent dual inhibitory action on MAGL and fatty acid amide hydrolase (FAAH). SAR629 inhibits rodent monoglyceride lipase (MGL) activity at subnanomolar potencies (IC50 values of 1.1 nM and 219 pM in rat and mouse brain membranes, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1221418-42-3
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Appearance Solid
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Molecular Weight 383.39
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Formel C20H19F2N5O
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Color White to off-white
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SMILES
O=C(N1N=CN=C1)N2CCN(CC2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (260.83 mM; Need ultrasonic; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Niina Aaltonen, et al. Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem Biol. 2013 Mar 21;20(3):379-90. [Content Brief]
[2]. T Bertrand, et al. Structural basis for human monoglyceride lipase inhibition. J Mol Biol. 2010 Feb 26;396(3):663-73. [Content Brief]
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 | 2.6083 mL | 13.0415 mL | 26.0831 mL | 65.2077 mL |
| 5 mM | 0.5217 mL | 2.6083 mL | 5.2166 mL | 13.0415 mL | |
| 10 mM | 0.2608 mL | 1.3042 mL | 2.6083 mL | 6.5208 mL | |
| 15 mM | 0.1739 mL | 0.8694 mL | 1.7389 mL | 4.3472 mL | |
| 20 mM | 0.1304 mL | 0.6521 mL | 1.3042 mL | 3.2604 mL | |
| 25 mM | 0.1043 mL | 0.5217 mL | 1.0433 mL | 2.6083 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8694 mL | 2.1736 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6521 mL | 1.6302 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5217 mL | 1.3042 mL | |
| 60 mM | 0.0435 mL | 0.2174 mL | 0.4347 mL | 1.0868 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8151 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6521 mL |