WS 3
WS 3 is an agonist of TRPM8 receptor with EC50 value of 3.7 μM [1].
Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a Ca2+- and Na+-permeable ion channel and is activated by cooling agents and cold temperatures. TRPM8 belongs to TRP family and is expressed in sensory neurons.
WS 3 is an agonist of TRPM8 receptor and a cooling agent. In HEK293 cells expressed recombinant mouse TRPM8, WS 3 (30 μM) increased [Ca2+]i. WS 3 exhibited potency with EC50 value of 3.7 μM and induced 86% efficacy of the maximal response to icilin, the most potent agonist [1]. In HEK cells stably expressing either hTRPM8 or hTRPA1, WS 3 activated hTRPM8 and hTRPA1 with EC50 values of 2.2 and 120.6 μM, respectively. WS 3 was efficacious in eliciting cooling sensation [2].
References:
[1]. Behrendt HJ, Germann T, Gillen C, et al. 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, 2004, 141(4): 737-745.
[2]. Klein AH, Iodi Carstens M, McCluskey TS, et al. Novel menthol-derived cooling compounds activate primary and second-order trigeminal sensory neurons and modulate lingual thermosensitivity. Chem Senses, 2011, 36(7): 649-658.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 569.58 |
| Cas No. | 1421227-52-2 |
| Formula | C28H30F3N7O3 |
| Solubility | insoluble in H2O; ≥15.37 mg/mL in EtOH with ultrasonic; ≥18.9 mg/mL in DMSO |
| Chemical Name | N-(6-(4-(3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide |
| SDF | Download SDF |
| Canonical SMILES | CN(CC1)CCN1CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=CC(NC(C5CC5)=O)=NC=N4)C=C3)=O)C=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
