Icilin

BML-CM126

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TRPM8 activator

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.

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Product Details

Alternative Name	AG 3-5, 3,6-Dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2(1H)-pyrimidinone
Appearance	Light yellow to orange solid.
CAS	36945-98-9
Couple Target	TRP channel
Couple Type	Activator
Formula	C₁₆H₁₃N₃O₄
MW	311.3
Purity	≥97% (TLC)
Solubility	Soluble in DMSO (50mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store, as supplied, at room temperature for up to 1 year. Store solutions at -20°C for up to 3 months.
Long Term Storage	Ambient
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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
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
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
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
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