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Product Details

Icilin | TRPM8 inhibitor

Icilin (36945-98-9) is an agonist of cold-sensitive TRP channels with 2.5-fold greater efficacy and 200-fold greater potency than menthol (EC50 = 0.36 μM for CRM1, rat orthologue of TRPM8).1 Agonist at TRPM8 (EC50 = 0.2 μM)2 and ANKTM1(TRPA1)3. Agonist effects require Ca2+ and are pH dependent.2,4 Icilin induced G1 arrest in PC-3 prostate cancer cells without cell death.5

References/Citations
1) McKemy et al. (2002) Identification of a cold receptor reveals a general role for TRP channels in thermosensation; Nature, 416 52
2) Andersson et al. (2004) TRPM8 activation by menthol, icilin and cold is differentially modulated by intracellular pH; J .Neurosci., 24 5364
3) Story et al. (2003) ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures; Cell, 112 819
4) Chuang et al. (2004) The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel; Neuron, 43 859
5) Kim et al. (2011) Icilin induces G1 arrest through activating JNK and p38 kinase in a TRPM8-independent manner; Biochem. Biophys. Res .Commun., 406 30

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Catalog#  10-4380

$65.00
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CAS:
36945-98-9
Catalog Number:
10-4380
Activity:
TRPM8 inhibitor
Alternate Names:
AG 3-5
Chemical Name:
3,6-Dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1H-pyrimidin-2-one
Molecular Weight:
311.29
Molecular Formula:
C16H13N3O4
Solubility:
Soluble in DMSO (up to 25 mg/ml),
Physical Properties:
Yellow solid
Purity:
>98% by TLC
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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