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Research tools

AR-231453

Reference GPR119 agonist (EC50 1.9 nM), the OEA receptor. Research tool, not a cannabinoid.

Unscheduled
Level of detail

C₂₁H₂₄FN₇O₅S

CAS 733750-99-7

Family
ECS pharmacological toolOther target
Molar mass
505.50 g/mol

Updated on

In plain terms

AR-231453 is not a cannabinoid: it is a laboratory molecule designed for diabetes research. It activates GPR119, a lipid sensor found in the gut and pancreas, which is also stimulated by lipids close to anandamide that the body makes. It has been studied in mice; no study in humans was found.

Receptors and activity

Target network

  • Activates

The lower the cited value, the closer the target sits to AR-231453: one ring per factor of 100. A target with no measured value stays on the edge.

Cited values

  1. GPR119AgonistEC50 = 1.9 nM79 out of 100

    Engelstoft et al., Br J Pharmacol 2014 (table 1, wild-type receptor, n = 26) (new tab) · cAMP accumulation, wild-type GPR119 transfected into COS7 cells (Emax 96%); the species of the construct is not stated explicitly, the paper models the human receptor (Q8TDV5); 0.68 nM in a melanophore assay on human GPR119 according to ChEMBL (Semple 2008 document)

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.

Measured effects

Not characterised. No placebo-controlled human trial has measured the effects of AR-231453, so no level is shown.

Levels computed from placebo-controlled human trials: difference from placebo on 100, at the dose and route stated. Read the method

Pharmacology

AR-231453 is the reference GPR119 agonist, described by the Arena Pharmaceuticals teams (Chu et al., Endocrinology 2007; Semple et al., J Med Chem 2008). GPR119 is not a cannabinoid receptor in the classical sense: it is a Gαs-coupled receptor activated by endogenous lipids such as oleoylethanolamide and 2-monoacylglycerol (Engelstoft et al. 2014); OEA was proposed as an endogenous GPR119 ligand in 2006 (Overton et al. 2006). At wild-type GPR119 expressed in COS7 cells (modelled on the human sequence), AR231453 acts with an EC50 of 1.9 nM and an efficacy of 96% (Engelstoft et al. 2014). In mice it increased glucose-dependent insulin release and improved oral glucose tolerance, effects absent in GPR119-deficient mice (Chu et al. 2007), then active GLP-1 within 2 minutes of an oral glucose load and total GIP (Chu et al. 2008). No activity at CB1 or CB2 was found; no study in humans was found.

Key sources.

History

Source
An entirely synthetic molecule from a medicinal chemistry programme at Arena Pharmaceuticals (San Diego) for diabetes; no natural source was found in the sources consulted. It is known as the reference GPR119 agonist in research.

Origin

Research tool

No known biosynthetic pathway: AR-231453 is a synthetic compound, a nitropyrimidine from medicinal chemistry, not described in any living organism (cannabis included).

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Other target

Verification

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

Wikipedia (English)

AR-231,453 (new tab)

Article paired by the molecule's structure (InChIKey), revision read on 19 October 2026. Read as a second opinion, never cited as a source.

References

  1. Chu ZL et al. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology, 2007 (new tab)PMID 17289847
  2. Semple G et al. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem, 2008 (new tab)PMID 18698756
  3. Chu ZL et al. A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glucose-dependent insulinotropic Peptide release. Endocrinology, 2008 (new tab)PMID 18202141
  4. Engelstoft MS et al. Structural basis for constitutive activity and agonist-induced activation of the enteroendocrine fat sensor GPR119. Br J Pharmacol, 2014 (new tab)PMID 25117266
  5. Overton HA et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab, 2006 (new tab)PMID 16517404
  6. PubChem, AR-231453, CID 24939268 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine
Other names
AR231453 · AR 231453 · AR-231,453 · CHEMBL461384

Identifiers

Formula
C₂₁H₂₄FN₇O₅S
CAS
733750-99-7
PubChem CID
24939268(new tab)
InChIKey
DGBKNTVAKIFYNU-UHFFFAOYSA-N
SMILES
CC(C)C1=NOC(=N1)C2CCN(CC2)C3=C(C(=NC=N3)NC4=C(C=C(C=C4)S(=O)(=O)C)F)[N+](=O)[O-]

Machine-readable entry (JSON)

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