Replaces Prod. #: ALX-420-037
Cooling agent. Strongly activates TRPM8 (IC50=0.2µM), cold menthol receptor 1 (CMR1, IC50=0.36µM), a nonselective, cold-activated cation channel and TRPA1 (at 10- to 100-fold higher concentration). Induces currents in TRPM8 expressing HEK 293 cells (EC50=0.36mM) more potently than menthol (Prod. No. ALX-420-042) or low temperatures. Activates TRPM8 with variable latency, followed by extensive desensitization provided calcium is present. The effects of icilin can be impacted by both pH and cytosolic calcium levels.
Product Details
| Alternative Name: | AG 3-5, 3,6-Dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2(1H)-pyrimidinone |
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| Formula: | C16H13N3O4 |
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| MW: | 311.3 |
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| CAS: | 36945-98-9 |
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| Purity: | ≥97% (TLC) |
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| Appearance: | Light yellow to orange solid. |
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| Solubility: | Soluble in DMSO (50mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | Ambient |
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| Use/Stability: | Store, as supplied, at room temperature for up to 1 year. Store solutions at -20°C for up to 3 months. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain: C.J. Proudfoot, et al.; Curr. Biol.
16, 1591 (2006),
Abstract;
Icilin activates the {delta}-subunit of the human epithelial Na+ channel.: H. Yamamura; Mol. Pharmacol.
68, 1142 (2005),
Abstract;
Sensing with TRP channels: T. Voets, et al.; Nat. Chem. Biol.
1, 85 (2005), Review,
Abstract;
Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay: H.J. Behrendt, et al.; Br. J. Pharmacol.
141, 737 (2004),
Abstract;
The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel: H.H. Chuang, et al.; Neuron
43, 859 (2004),
Abstract;
TRPM8 activation by menthol, icilin, and cold is differentially modulated by intracellular pH: D.A. Andersson, et al.; J. Neurosci.
24, 5364 (2004),
Abstract;
Full Text
ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures: G.M. Story, et al.; Cell
112, 819 (2003),
Abstract;
Identification of a cold receptor reveals a general role for TRP channels in thermosensation: D.D. McKemy, et al.; Nature
416, 52 (2002),
Abstract;
AG-3-5: a chemical producing sensations of cold: E.T. Wei and D.A. Seid; J. Pharm. Pharmacol.
35, 110 (1983),
Abstract;
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