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Research tools

SAR127303

A covalent MAGL inhibitor designed by Sanofi, a research tool with no human data.

Unscheduled
Level of detail

Harm-reduction warning

No characterised human dose: animal / in vitro data only. Effect profile, safety margin and acute toxicity are not documented in human clinical practice. Extremely potent compound: severe effects, seizures and deaths reported in the literature.

C₁₆H₁₇ClF₆N₂O₄S

CID 54761543

Family
ECS pharmacological toolEnzyme inhibitor
Molar mass
482.80 g/mol

Updated on

In plain terms

SAR127303 is a laboratory molecule developed by a pharmaceutical group, with no connection to hemp. It blocks a brain enzyme that destroys a cannabinoid the body makes itself, 2-AG, which makes the level of the latter rise. No study in humans was found and it is not a consumer product.

Receptors and activity

Target network

MAGL (monoacylglycerol lipase)InhibitorIC50 = 29 nM · humanenzymatic, human MAGL, covalent and competitive inhibition; 3.8 nM on mouse MAGL, 48 nM on recombinant human MAGL (4-nitrophenyl acetate substrate)
  • Blocks or inhibits

The lower the cited value, the closer the target sits to SAR127303: one ring per factor of 100. A target with no measured value stays on the edge.

Where these targets live

Where each target has been found in humans, according to the cited studies. The map shows the target, not an effect of SAR127303.

Brain, side view
Body, front view
Blood

MAGLMAGL found in 5 regions of the body

  1. CortexdenseHighest PET signal in the cerebral cortex1
  2. Basal gangliapresentModerate levels in the putamen1
  3. HippocampuspresentAxon terminals in the hippocampus2
  4. Adipose tissuepresentPresent in subcutaneous adipose tissue3
  5. Immune cellspresentRNA enhanced in blood monocytes4

Map sources

  1. Takahata K et al. First-in-human in vivo imaging and quantification of monoacylglycerol lipase in the brain: a PET study with (18)F-T-401. Eur J Nucl Med Mol Imaging, 2022 (new tab)
  2. Ludányi A et al. Complementary synaptic distribution of enzymes responsible for synthesis and inactivation of the endocannabinoid 2-arachidonoylglycerol in the human hippocampus. Neuroscience, 2011 (new tab)
  3. Spoto B et al. Human adipose tissue binds and metabolizes the endocannabinoids anandamide and 2-arachidonoylglycerol. Biochimie, 2006 (new tab)
  4. Human Protein Atlas. MGLL expression summary (new tab)

Cited values

  1. MAGL (monoacylglycerol lipase)InhibitorIC50 = 29 nM · human59 out of 100

    Griebel et al., Sci Rep 2015 (new tab) · enzymatic, human MAGL, covalent and competitive inhibition; 3.8 nM on mouse MAGL, 48 nM on recombinant human MAGL (4-nitrophenyl acetate substrate)

  2. ABHD6Inhibitorno measured value cited

    The only other human serine hydrolase whose activity was altered in the panel tested; no numerical value in the text (Griebel et al. 2015)

Bar length follows the measured value (Ki, Kd, EC50 or IC50), on one scale shared by every entry, from 100 µM to 0.1 nM. A target with no cited value has no bar.

Pharmacology

SAR127303 is a carbamate described in 2015 by Sanofi as a selective, competitive, covalent inhibitor of monoacylglycerol lipase (MAGL), the enzyme that degrades 2-arachidonoylglycerol. Its IC50 is 3.8 nM on mouse MAGL and 29 nM on human MAGL; mass spectrometry identified the catalytic serine as the covalent binding site, and the structure of the complex with human MAGL (code 4UUQ) shows the hexafluoropropan-2-ol leaving during catalysis (Griebel et al. 2015). Given orally to mice, peak plasma and brain concentrations are reached at 4 hours, brain MAGL activity is markedly inhibited for up to 6 hours, and hippocampal 2-AG rises about 30-fold with no change in anandamide, PEA or OEA. The cannabinoid tetrad (tail-flick antinociception, catalepsy, hypothermia, reduced locomotor activity) was not observed up to 30 mg/kg. In rodents the compound produced antinociceptive effects in inflammatory and visceral pain tests and, given repeatedly, delayed the acquisition of kindled seizures; but it also impaired learning (episodic, working and spatial memory) and decreased long-term potentiation at CA1 synapses and hippocampal acetylcholine release. The authors conclude that blocking 2-AG hydrolysis may have limited therapeutic value. The carbon-11 labelled form was evaluated as a MAGL tracer in rats and a non-human primate (Wang et al. 2016). No study in humans was found.

Key sources.

History

Source
An entirely synthetic molecule with no known natural occurrence, not derived from hemp. It was developed by Sanofi as an inhibitor of MAGL (Griebel et al. 2015), then radiolabelled with carbon-11 as a positron emission tomography imaging tracer (Wang et al. 2016).

Origin

Research tool

No biosynthetic pathway: it is a synthetic chemical compound, built around a piperidine carbamate combined with a chlorinated sulfonamide motif and a hexafluoropropan-2-yl ester. No plant, animal or human enzyme produces it, and it appears in no natural metabolic pathway.

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Enzyme inhibitor

Verification

Classification, sources and binding values checked on 20 October 2026; text read against its sources and Wikipedia.

Wikipedia (English)

No dedicated article.

References

  1. Griebel G et al. Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents. Sci Rep, 2015 (new tab)PMID 25560837
  2. RCSB PDB 4UUQ, crystal structure of human monoglyceride lipase in complex with SAR127303, resolution 2.36 Å (deposited 30/07/2014) (new tab)
  3. Wang L et al. Synthesis and preclinical evaluation of sulfonamido-based [11C-carbonyl]-carbamates and ureas for imaging monoacylglycerol lipase. Theranostics, 2016 (new tab)PMID 27279908
  4. PubChem, SAR127303, CID 54761543 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[(4-chlorophenyl)sulfonylamino]methyl]piperidine-1-carboxylate
Other names
SAR-127303 · MAGL-IN-12

Identifiers

Formula
C₁₆H₁₇ClF₆N₂O₄S
PubChem CID
54761543(new tab)
InChIKey
RLYMQNQYCHGICP-UHFFFAOYSA-N
SMILES
C1CN(CCC1CNS(=O)(=O)C2=CC=C(C=C2)Cl)C(=O)OC(C(F)(F)F)C(F)(F)F

Machine-readable entry (JSON)

LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.