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ECS modulator (research)

Unscheduled

URB597URB597 (KDS-4103)

[3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate

Aliases.KDS-4103 · Carbamic acid 3'-(aminocarbonyl)biphenyl-3-yl ester

The reference FAAH inhibitor. The standard pharmacological tool for studying endogenous AEA in vivo.

Updated on

Level of detail

Identifiers

Formula
C₂₀H₂₂N₂O₃
Molar mass
338.40 g·mol⁻¹
CAS
546141-08-6
PubChem CID
1383884
First described
2003
Origin
Pharmaceutical research (Piomelli)
InChIKey
ROFVXGGUISEHAM-UHFFFAOYSA-N

In plain terms

URB597 is an experimental drug that prevents the body from destroying its own anandamide. It has been tested in humans for pain and anxiety, but has never been marketed.

Receptors and activity

  • FAAH
    IC50 ≈ 4,6 nM (rat)Antagonist
  • CB1
    indirect via AEAModulator
  • Agonist
  • Partial agonist
  • Antagonist
  • Modulator
  • Inverse agonist

Hover over a row for the precise value (Ki, EC50…)

Subjective signature

Hover over an axis to read its definition.

  • Calm
    75
  • Clarity
    45
  • Sleep
    55
  • Appetite
    40
  • High
    50

Editorial estimate, not clinical.

Pharmacology

URB597 is the reference FAAH inhibitor - characterised by Kathuria, Mor, Mangieri and Piomelli (Nat Med 2003, PMID 12514735) at the University of California. Covalent mechanism: irreversible carbamylation of Ser241 in the active site of FAAH. Anxiolytic and antidepressant effect in rodent models (Bortolato et al. 2007, PMID 16968671). Human phase 2 for neuropathic pain and anxiety: abandoned in 2008 after the BIA 10-2474 incident (another FAAH inhibitor), even though URB597 itself never showed similar neurotoxicity.

Origin (research tool)

An irreversible covalent inhibitor of FAAH; obtained by organic synthesis (carbamylation of the Ser241 residue of the active site)

Structural classification

Class
ECS modulator (research)
Origin
Pharmaceutical research (Piomelli)
Status
Unscheduled

References

  1. 1.Kathuria · Nat Med 2003PMID 12514735

Structured data

InChIKey
ROFVXGGUISEHAM-UHFFFAOYSA-N
SMILES
C1CCC(CC1)NC(=O)OC2=CC=CC(=C2)C3=CC(=CC=C3)C(=O)N
Formula
C20H22N2O3
Molar mass
338.40 g·mol⁻¹
CAS
546141-08-6
PubChem CID
1383884
Machine-readable entry (JSON)

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