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Research tools

JD5037

Peripherally restricted CB1 blocker, studied in mice; preclinical 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.

C₂₇H₂₇Cl₂N₅O₃S

CAS 1392116-14-1

Family
ECS pharmacological toolAntagonist or inverse agonist
Molar mass
572.50 g/mol

Updated on

In plain terms

JD5037 is a laboratory molecule with no link to hemp: it blocks the CB1 receptor, the one THC activates. It was designed to act in the body without reaching the brain, to avoid the neuropsychiatric effects that led first-generation CB1 blockers to be abandoned. In mice made obese, it reduced body weight and fatty liver; the data cited are preclinical.

Receptors and activity

Target network

CB1Inverse agonistKi = 0.4 nMCB1 binding affinity; inverse agonist verified by GTPγS binding; species not specified in the cited text
  • Blocks or inhibits
  • Binds or modulates

The lower the cited value, the closer the target sits to JD5037: 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 JD5037.

Brain, side view
Body, front view
Blood

CB1CB1 found in 7 regions of the body

  1. Basal gangliadenseMost dense in basal ganglia outflow nuclei1
  2. CerebellumdenseVery dense in the cerebellum1
  3. HippocampusdenseVery high concentrations in the hippocampus2
  4. AmygdaladenseHigh concentrations in the amygdala2
  5. CortexpresentPresent throughout the neocortex2
  6. Adipose tissuepresentExpressed in adipose tissue3
  7. GutpresentColonic epithelium, smooth muscle and plexus4

Map sources

  1. Herkenham M et al. Cannabinoid receptor localization in brain. Proc Natl Acad Sci U S A, 1990 (new tab)
  2. Glass M et al. Cannabinoid receptors in the human brain: a detailed anatomical and quantitative autoradiographic study in the fetal, neonatal and adult human brain. Neuroscience, 1997 (new tab)
  3. Engeli S et al. Activation of the peripheral endocannabinoid system in human obesity. Diabetes, 2005 (new tab)
  4. Wright K et al. Differential expression of cannabinoid receptors in the human colon: cannabinoids promote epithelial wound healing. Gastroenterology, 2005 (new tab)

Cited values

  1. CB1Inverse agonistKi = 0.4 nM91 out of 100

    Tam et al., Cell Metab 2012 (new tab) · CB1 binding affinity; inverse agonist verified by GTPγS binding; species not specified in the cited text

  2. CB1Inverse agonistIC50 = 0.5 nM · human88 out of 100

    Chorvat et al., Bioorg Med Chem Lett 2012 (ChEMBL value) (new tab) · displacement of a tritiated ligand at recombinant human CB1

  3. CB2Binding (function not established)no measured value cited
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

JD5037 is a peripherally restricted inverse agonist of the CB1 receptor, derived from ibipinabant (SLV-319) (Chorvat et al. 2012). Its Ki at CB1 is 0.35 nM, with a selectivity of more than 700-fold over CB2 (Tam et al. 2012). In mice, the brain-to-plasma ratio is below 2% after a single oral dose of 3 mg/kg and about 7% after 28 days, and positron emission tomography showed no occupancy of brain CB1 receptors. In mice made obese by diet, 3 mg/kg/day orally for 28 days reduced food intake, body weight, adiposity and hepatic steatosis, and normalised blood glucose and insulin to a similar degree as ibipinabant, with tolerance to the anorexic effect appearing after 14 days. According to Tam et al., the fall in food intake and weight runs through reversal of hyperleptinaemia (lower leptin expression and secretion by adipocytes, increased renal clearance): in ob/ob and db/db mice, JD5037 did not change food intake, body weight or adiposity, whereas some metabolic parameters changed similarly. Other mouse studies reported a fall in ethanol intake linked to reduced formation of active ghrelin (Godlewski et al. 2019) and a suppression of food intake independent of the vagal axis (Onimus et al. 2026). Conversely, in Mdr2-/- mice with established liver fibrosis, four weeks of treatment worsened liver injury (Chen et al. 2024). All these data are preclinical.

Key sources.

History

Source
A synthetic molecule derived from ibipinabant (SLV-319), absent from hemp and from any living organism. A preclinical drug candidate for visceral obesity and its metabolic complications, used as a research reagent.

Origin

Research tool

No biosynthetic pathway: a synthetic molecule of the diarylpyrazoline class, derived from ibipinabant.

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Antagonist or inverse agonist

Verification

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

Wikipedia (English)

JD5037 (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. Chorvat RJ, Berbaum J, Seriacki K, McElroy JF, JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities, Bioorg Med Chem Lett 2012 (new tab)PMID 22959249
  2. Tam J et al., Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance, Cell Metab 2012;16(2):167-179 (new tab)PMID 22841573
  3. Kale VP et al., Preclinical toxicity evaluation of JD5037, a peripherally restricted CB1 receptor inverse agonist, in rats and dogs for treatment of nonalcoholic steatohepatitis, Regul Toxicol Pharmacol 2019 (new tab)PMID 31580887
  4. Godlewski G et al., Targeting Peripheral CB1 Receptors Reduces Ethanol Intake via a Gut-Brain Axis, Cell Metab 2019 (new tab)PMID 31105045
  5. Chen J et al., Peripherally Restricted CB1 Receptor Inverse Agonist JD5037 Treatment Exacerbates Liver Injury in MDR2-Deficient Mice, Cells 2024 (new tab)PMID 38994954
  6. Onimus O et al., Inhibition of peripheral CB1 receptors modulates food intake and metabolic efficiency in obesity independently of the gut-brain vagal axis, Br J Pharmacol 2026 (new tab)PMID 42155998
  7. Cinar R, Iyer MR, Kunos G, The therapeutic potential of second and third generation CB1R antagonists, Pharmacol Ther 2020 (new tab)PMID 31926199
  8. ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
  9. PubChem, compound CID 66553204 (JD-5037) (new tab)

Identifiers

Names

IUPAC name
(2S)-2-[[[(4S)-5-(4-chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-[(4-chlorophenyl)sulfonylamino]methylidene]amino]-3-methylbutanamide
Other names
JD-5037 · JD 5037

Identifiers

Formula
C₂₇H₂₇Cl₂N₅O₃S
CAS
1392116-14-1
PubChem CID
66553204(new tab)
InChIKey
GTCSIQFTNPTSLO-RPWUZVMVSA-N
SMILES
CC(C)[C@@H](C(=O)N)N=C(NS(=O)(=O)C1=CC=C(C=C1)Cl)N2C[C@@H](C(=N2)C3=CC=C(C=C3)Cl)C4=CC=CC=C4

Machine-readable entry (JSON)

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