ART26.12
Synthetic FABP5 inhibitor (Ki 0.77 µM), the anandamide shuttle: preclinical data and a phase 1 study announced by the company.
C₂₉H₂₈O₆
CID 163249803
- Family
- ECS pharmacological toolTransport inhibitor
- Molar mass
- 472.50 g/mol
Updated on
In plain terms
ART26.12 is a laboratory-made molecule: it does not exist in hemp and behaves neither like CBD nor like THC. Instead of binding a cannabinoid receptor, it blocks a small protein called FABP5, which carries lipids such as anandamide inside cells. In rats it reduced pain hypersensitivity in several neuropathy models; the company developing it announces a phase 1 study in healthy volunteers.
Receptors and activity
Target network
- Blocks or inhibits
The lower the cited value, the closer the target sits to ART26.12: one ring per factor of 100. A target with no measured value stays on the edge.
Cited values
- FABP5 (transporteur intracellulaire de l'anandamide)InhibitorKi = 770 nM35 out of 100
Warren et al., J Pain 2024 (full text, Europe PMC) (new tab) · fluorescence displacement assay (DAUDA) on purified FABP5 (0.77 ± 0.08 µM); selectivity of about 93-fold over FABP3 and 25-fold over FABP7; species not specified in the passage read
- FABP7InhibitorKi = 19 µM12 out of 100
Warren et al., J Pain 2024 (full text, Europe PMC) (new tab) · fluorescence displacement assay (ANS) on purified FABP7 (18.99 ± 1.81 µM); species not specified in the passage read
- FABP3InhibitorKi = 71.3 µM4 out of 100
Warren et al., J Pain 2024 (full text, Europe PMC) (new tab) · fluorescence displacement assay (DAUDA) on purified FABP3 (71.32 ± 2.40 µM); species not specified in the passage read
- FABP4Inhibitorno measured value cited
Ki greater than 100 µM (Warren et al. 2024)
Measured effects
Not characterised. No placebo-controlled human trial has measured the effects of ART26.12, 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
ART26.12 is not a cannabinoid but a selective inhibitor of FABP5, a fatty acid-binding protein that carries lipids such as anandamide inside the cell. Its Ki is 0.77 µM at FABP5, 18.99 µM at FABP7, 71.32 µM at FABP3 and above 100 µM at FABP4 (Warren et al. 2024). In rats, given orally, it reversed mechanical allodynia in an oxaliplatin neuropathy model (25 to 100 mg/kg; effect reduced by the CB1 antagonist AM251) and prevented the onset of thermal hyperalgesia when given with oxaliplatin (10 and 25 mg/kg twice daily for 15 days) (Warren et al. 2024); it also reversed allodynia in paclitaxel neuropathy, streptozotocin diabetic neuropathy and breast cancer-induced bone pain models (Warren et al. 2025). In an imiquimod psoriasis model in mice it reduced symptom severity (Warren et al. 2025, J Invest Dermatol). 14-day repeated-dose toxicity studies in rats and dogs established a no-observed-adverse-effect level of 1,000 mg/kg/day. These studies, funded and carried out by Artelo Biosciences, which is developing the molecule, are preclinical. According to company press releases (13 January 2025 and 29 June 2026), a single-ascending-oral-dose phase 1 study in healthy volunteers has been conducted and described as generally well tolerated at all dose levels evaluated, with dose-proportional exposure; these data do not appear in a peer-reviewed publication among the sources consulted, and no efficacy in humans is established.
Key sources.
- Warren G et al. Discovery and Preclinical Evaluation of a Novel Inhibitor of FABP5, ART26.12, Effective in Oxaliplatin-Induced Peripheral Neuropathy. J Pain, 2024 (new tab)PMID 38232863
- Warren WG et al. ART26.12, a novel fatty acid-binding protein 5 inhibitor, shows efficacy in multiple preclinical neuropathy models. Eur J Pain, 2025 (new tab)PMID 39188040
- Warren WG et al. Potential safety implications of fatty acid-binding protein inhibition. Toxicol Appl Pharmacol, 2024 (new tab)PMID 39218163
- Warren WG et al. ART26.12, an FABP5 Inhibitor, Shows Efficacy in Preclinical Psoriasis Models. J Invest Dermatol, 2025 (new tab)PMID 40210114
- Artelo Biosciences, press release of 13 January 2025: completion of the first cohort of a phase 1 study of ART26.12 (source: company) (new tab)
- Artelo Biosciences, press release of 29 June 2026: clinical and biomarker data presented at ICRS 2026 (source: company) (new tab)
- PubChem, ART26.12, CID 163249803 (identifiers and properties) (new tab)
History
- Source
- An entirely synthetic molecule from a pharmaceutical programme at Artelo Biosciences on truxillic acid monoesters; it is not a cannabis product and no natural occurrence was found. The company is developing it as a drug candidate (Warren et al. 2024); it does not circulate as a consumer product.
Origin
Research tool
No known biological pathway: ART26.12 is a synthetic compound of the truxillic acid monoester family (diaryl-substituted cinnamic acid dimers) esterified with indan-2-ol; to our knowledge no plant or organism produces it.
Legal framework
- European Union
The substance is not listed in the Annex to Council Framework Decision 2004/757/JHA (consolidated version of 12 January 2026), which lists the new psychoactive substances controlled at European Union level; control is a matter for national law. It is not listed in the schedules of the 1971 Convention on Psychotropic Substances (INCB Green List, 36th edition, 2025, text reviewed). No marketing authorisation was found: the molecule is a drug candidate in development.
- France
Not classified: ART26.12 is not on the ANSM consolidated list of narcotics (updated 16/02/2026) and this truxillic acid monoester, with no cannabinoid, indole, indazole or benzo[c]chromene core, falls within none of the generic families of that list. No marketing authorisation was found: the molecule is a drug candidate in development.
Sources: EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA. Our method.
Classification
Family, origin and source verification
- Family
ECS pharmacological tool › Transport 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
- Warren G et al. Discovery and Preclinical Evaluation of a Novel Inhibitor of FABP5, ART26.12, Effective in Oxaliplatin-Induced Peripheral Neuropathy. J Pain, 2024 (new tab)PMID 38232863
- Warren WG et al. ART26.12, a novel fatty acid-binding protein 5 inhibitor, shows efficacy in multiple preclinical neuropathy models. Eur J Pain, 2025 (new tab)PMID 39188040
- Warren WG et al. Potential safety implications of fatty acid-binding protein inhibition. Toxicol Appl Pharmacol, 2024 (new tab)PMID 39218163
- Warren WG et al. ART26.12, an FABP5 Inhibitor, Shows Efficacy in Preclinical Psoriasis Models. J Invest Dermatol, 2025 (new tab)PMID 40210114
- Artelo Biosciences, press release of 13 January 2025: completion of the first cohort of a phase 1 study of ART26.12 (source: company) (new tab)
- Artelo Biosciences, press release of 29 June 2026: clinical and biomarker data presented at ICRS 2026 (source: company) (new tab)
- PubChem, ART26.12, CID 163249803 (identifiers and properties) (new tab)
Identifiers
Names
- IUPAC name
- trans-(2R,4R)-3-(2,3-dihydro-1H-inden-2-yloxycarbonyl)-2,4-bis(2-methoxyphenyl)cyclobutane-1-carboxylic acid
Identifiers
- Formula
- C₂₉H₂₈O₆
- PubChem CID
- 163249803(new tab)
- InChIKey
- HFKXLDACQCGGEI-BINWOUKTSA-N
- SMILES
- COC1=
CC= CC= C1[C@@H] 2C([C@H] (C2C(= O) OC3CC4= CC= CC= C4C3) C5= CC= CC= C5OC) C(= O) O
LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.