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Research tools

AS-1269574

Partial GPR119 agonist (EC50 2.5 µM) that also activates TRPA1; no activity at CB1 or CB2 found.

Unscheduled
Level of detail

C₁₃H₁₄BrN₃O

CID 5332859

Family
ECS pharmacological toolOther target
Molar mass
308.17 g/mol

Updated on

In plain terms

AS-1269574 is a laboratory molecule, identified in 2010 for diabetes research. It does not exist in hemp and has nothing in common with CBD: it acts on GPR119, a receptor close to the endocannabinoid system that normally responds to lipids made by the gut. In mice it increased insulin secretion when blood sugar was high; no study in humans was found.

Receptors and activity

Target network

TRPA1AgonistDirect activation, independent of GPR119 and of cAMP, in the STC-1 line and in HEK293 cells expressing rat TRPA1 without GPR119; inhibited by AP-18, A967079 and HC030031; value not given in the abstract (Chepurny et al. 2016)
  • Activates

The lower the cited value, the closer the target sits to AS-1269574: 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 AS-1269574.

Brain, side view
Body, front view
Blood

TRPA1TRPA1 found in 4 regions of the body

  1. Sensory gangliapresentDorsal root ganglion neurons1
  2. Spinal cordpresentSpinal cord motor neurons1
  3. GutpresentIntestinal myenteric plexus neurons1
  4. SkinpresentBasal keratinocytes of the skin1

Map sources

  1. Anand U et al. TRPA1 receptor localisation in the human peripheral nervous system and functional studies in cultured human and rat sensory neurons. Neurosci Lett, 2008 (new tab)

Cited values

  1. GPR119Partial agonistEC50 = 2.5 µM · human27 out of 100

    Yoshida et al., Biochem Biophys Res Commun 2010 (new tab) · human GPR119 transiently expressed in HEK293 cells, CRE-luciferase reporter (2.5 µM); partial agonist according to the cryo-EM structure of Zhang 2026

  2. TRPA1Agonistno measured value cited

    Direct activation, independent of GPR119 and of cAMP, in the STC-1 line and in HEK293 cells expressing rat TRPA1 without GPR119; inhibited by AP-18, A967079 and HC030031; value not given in the abstract (Chepurny et al. 2016)

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 AS-1269574, 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

AS-1269574 is a synthetic GPR119 agonist, a Gαs-coupled receptor activated by lipids such as oleoylethanolamide and 2-monoacylglycerol, which places it at the periphery of the endocannabinoid system without making it a cannabinoid. At human GPR119 expressed in HEK293 cells its potency is modest (EC50 2.5 µM); a cryo-EM structure published in 2026 describes it as a partial agonist (Zhang et al. 2026). In normal mice a single administration reduced blood glucose after an oral glucose load without changing fasting or fed plasma glucose (Yoshida et al. 2010); in streptozotocin-induced diabetic mice, daily oral treatment for 28 days (0.1 µmol/kg) lowered plasma glucose by 20 to 26% and raised circulating insulin by 47 to 48% (McKillop et al. 2016); in rats, intrathecal administration produced a dose-dependent antiallodynic effect in a spinal nerve ligation model (Zúñiga-Romero et al. 2022). A second mechanism complicates the picture: GLP-1 release in the STC-1 line was attributed in 2016 to direct activation of the TRPA1 channel, independently of GPR119, an effect not reproduced by AR231453 or oleoylethanolamide; the authors speak of a dual GPR119/TRPA1 agonist (Chepurny et al. 2016). No activity at CB1 or CB2 was found. These are preclinical results; no study in humans was found.

Key sources.

History

Source
An entirely synthetic molecule, identified by screening a library of synthetic compounds (Yoshida et al. 2010); no natural occurrence was found in the sources consulted. It is known as a laboratory pharmacological tool used to probe the GPR119 receptor.

Origin

Research tool

No biological pathway: AS-1269574 is a synthetic compound of the 4-amino-2-phenylpyrimidine series of GPR119 agonists, not described in any living organism.

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)

No dedicated article.

References

  1. Yoshida S et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem Biophys Res Commun, 2010 (new tab)PMID 20804735
  2. Negoro K et al. Synthesis and structure-activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists. Bioorg Med Chem, 2012 (new tab)PMID 22365911
  3. Chepurny OG et al. GPR119 agonist AS1269574 activates TRPA1 cation channels to stimulate GLP-1 secretion. Mol Endocrinol, 2016 (new tab)PMID 27082897
  4. McKillop AM et al. Metabolic effects of orally administered small-molecule agonists of GPR55 and GPR119 in multiple low-dose streptozotocin-induced diabetic and incretin-receptor-knockout mice. Diabetologia, 2016 (new tab)PMID 27677765
  5. Zúñiga-Romero Á et al. GPR55 and GPR119 receptors contribute to the processing of neuropathic pain in rats. Pharmaceuticals (Basel), 2022 (new tab)PMID 35056124
  6. Zhang Y et al. An extracellular allosteric gate modulates the ligand efficacy of GPR119. Structure, 2026 (new tab)PMID 42269610
  7. PubChem, AS-1269574, CID 5332859 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
2-[[2-(4-bromophenyl)-6-methylpyrimidin-4-yl]amino]ethanol
Other names
AS1269574 · AS 1269574

Identifiers

Formula
C₁₃H₁₄BrN₃O
PubChem CID
5332859(new tab)
InChIKey
DUKPGOOUJNUIOI-UHFFFAOYSA-N
SMILES
CC1=CC(=NC(=N1)C2=CC=C(C=C2)Br)NCCO

Machine-readable entry (JSON)

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