2. Metabolic Enzyme/Protease
  3. MAGL
  4. SAR629

SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation.

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SAR629 Chemical Structure

SAR629 Chemical Structure

CAS No. : 1221418-42-3

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Based on 1 publication(s) in Google Scholar

SAR629 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation[1][2].

Cellular Effect
Cell Line Type Value Description References
COS-7 IC50
282 nM
Compound: SAR629
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
[PMID: 25282655]
HEK293 IC50
0.9 nM
Compound: SAR629
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
[PMID: 25282655]
In Vitro

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.

SAR629 Related Antibodies
Molecular Weight

383.39

Formula

C20H19F2N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1N=CN=C1)N2CCN(CC2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6083 mL 13.0415 mL 26.0831 mL
5 mM 0.5217 mL 2.6083 mL 5.2166 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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
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SAR629 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAR6291221418-42-3SAR 629SAR-629MAGLMonoacylglycerol lipasemonoglyceridelipaseMGLFAAHInhibitorinhibitorinhibit

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