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Description: Activates cold receptors. Cooling agent
Alternative Names: AG 3-5
Chemical Name: 3,4-Dihydro-3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-(1H)-pyrimidin-2-one
Purity: ≥98% (HPLC)
Citations (5)

Biological Activity for Icilin

Icilin is a cooling agent that activates the novel cold receptors TRPM8 (CMR1) and TRPA1 (ANKTM1/TRPN1), members of the TRP ion channel family. Induces currents in CMR1-expressing HEK 293 cells (EC50 = 0.36 μM) more potently than menthol or low temperatures. Produces "wet shakes" in vivo.

Technical Data for Icilin

M. Wt 311.3
Formula C16H13N3O4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 36945-98-9
PubChem ID 161930
Smiles OC1=C(C=CC=C1)N1CC=C(NC1=O)C1=CC=CC(=C1)[N+]([O-])=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Icilin

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 31.13 100

Preparing Stock Solutions for Icilin

The following data is based on the product molecular weight 311.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.21 mL 16.06 mL 32.12 mL
5 mM 0.64 mL 3.21 mL 6.42 mL
10 mM 0.32 mL 1.61 mL 3.21 mL
50 mM 0.06 mL 0.32 mL 0.64 mL

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Product Datasheets for Icilin

Certificate of Analysis / Product Datasheet
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References for Icilin

References are publications that support the biological activity of the product.

Behrendt et al (2004) Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br.J.Pharmacol. 141 737 PMID: 14757700

McKemy et al (2002) Identification of a cold receptor reveals a general role for TRP channels in thermosensation. Nature 416 52 PMID: 11882888

Story et al (2003) ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures. Cell 112 819 PMID: 12654248

Wei et al (1983) AG-3-5: a chemical producing sensations of cold. J.Pharm.Pharmacol. 35 110 PMID: 6131976

Diver et al (2019) Science.

If you know of a relevant reference for Icilin, please let us know.

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Keywords: Icilin, Icilin supplier, activators, novel, cold, receptor, Cooling, agent, TRP, Channels, Transient, Receptor, Potential, AG35, TRPA, TRPM, AG, 3-5, TRPA1, 1531, Tocris Bioscience

5 Citations for Icilin

Citations are publications that use Tocris products. Selected citations for Icilin include:

Ganley et al (2015) Inhibitory Interneurons That Express GFP in the PrP-GFP Mouse Spinal Cord Are Morphologically Heterogeneous, Innervated by Several Classes of Primary Afferent and Include Lamina I Projection Neurons among Their Postsynaptic Targets. Oncogene 35 7626 PMID: 25972186

Gkika et al (2010) PSA reduces prostate cancer cell motility by stimulating TRPM8 activity and plasma membrane expression. Respir Res 29 4611 PMID: 20531306

Knowlton et al (2011) Pharmacological blockade of TRPM8 ion channels alters cold and cold pain responses in mice. PLoS One 6 e25894 PMID: 21984952

Diver et al (2019) Structural insights into TRPM8 inhibition and desensitization. Science 365 1434 PMID: 31488702

Proudfoot et al (2006) Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr Biol 16 1591 PMID: 16920620

Do you know of a great paper that uses Icilin from Tocris? Please let us know.

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