WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H555191
CAS#: 1352011-38-1
Description: SAR127303 is a potent covalent MAGL inhibitor. SAR127303 behaves as a selective and competitive inhibitor of mouse and human MAGL, which potently elevates hippocampal levels of 2-AG in mice. In vivo, SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain.
Hodoodo Cat#: H555191
Name: SAR127303
CAS#: 1352011-38-1
Chemical Formula: C16H17ClF6N2O4S
Exact Mass: 482.05
Molecular Weight: 482.822
Elemental Analysis: C, 39.80; H, 3.55; Cl, 7.34; F, 23.61; N, 5.80; O, 13.25; S, 6.64
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Synonym: SAR127303; SAR-127303; SAR 127303.
IUPAC/Chemical Name: 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(((4-chlorophenyl)sulfonamido)methyl)piperidine-1-carboxylate
InChi Key: RLYMQNQYCHGICP-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H17ClF6N2O4S/c17-11-1-3-12(4-2-11)30(27,28)24-9-10-5-7-25(8-6-10)14(26)29-13(15(18,19)20)16(21,22)23/h1-4,10,13,24H,5-9H2
SMILES Code: ClC1=CC=C(S(NCC2CCN(C(OC(C(F)(F)F)C(F)(F)F)=O)CC2)(=O)=O)C=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Monoacylglycerol lipase (MAGL) represents a primary degradation enzyme of the endogenous cannabinoid (eCB), 2-arachidonoyglycerol (2-AG).
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 482.82 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 | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Wang L, Mori W, Cheng R, Yui J, Hatori A, Ma L, Zhang Y, Rotstein BH, Fujinaga
M, Shimoda Y, Yamasaki T, Xie L, Nagai Y, Minamimoto T, Higuchi M, Vasdev N,
Zhang MR, Liang SH. Synthesis and Preclinical Evaluation of Sulfonamido-based
[(11)C-Carbonyl]-Carbamates and Ureas for Imaging Monoacylglycerol Lipase.
Theranostics. 2016 May 21;6(8):1145-59. doi: 10.7150/thno.15257. eCollection
2016. PubMed PMID: 27279908; PubMed Central PMCID: PMC4893642.
2: Wang C, Placzek MS, Van de Bittner GC, Schroeder FA, Hooker JM. A Novel
Radiotracer for Imaging Monoacylglycerol Lipase in the Brain Using Positron
Emission Tomography. ACS Chem Neurosci. 2016 Apr 20;7(4):484-9. doi:
10.1021/acschemneuro.5b00293. Epub 2016 Jan 6. PubMed PMID: 26694017.
3: Griebel G, Pichat P, Beeské S, Leroy T, Redon N, Jacquet A, Françon D, Bert L,
Even L, Lopez-Grancha M, Tolstykh T, Sun F, Yu Q, Brittain S, Arlt H, He T, Zhang
B, Wiederschain D, Bertrand T, Houtmann J, Rak A, Vallée F, Michot N, Augé F,
Menet V, Bergis OE, George P, Avenet P, Mikol V, Didier M, Escoubet J. Selective
blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs
learning and memory performance while producing antinociceptive activity in
rodents. Sci Rep. 2015 Jan 6;5:7642. doi: 10.1038/srep07642. PubMed PMID:
25560837; PubMed Central PMCID: PMC4284516.