| CAS NO: | 1421227-52-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 200mg | 电议 |
| 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 |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
WS 3是一种TRPM8受体激动剂,EC50值为3.7 μM [1].
瞬时受体电位阳离子通道亚家族M成员8(TRPM8)是一种Ca2+和Na+通透的离子通道,可被冷却剂和低温激活.TRPM8属于TRP家族,在感觉神经元上表达.
WS 3是一种TRPM8受体的激动剂,也是一种冷却剂.在表达重组小鼠TRPM8的HEK293细胞中,WS 3 (30 μM)增加[Ca2+]i含量.WS 3具有EC50值为3.7 μM的效力,诱发对icilin(最强效的激动剂)最大效应的86%的效力[1].在稳定表达hTRPM8或hTRPA1的HEK细胞中,WS 3激活hTRPM8和hTRPA1,EC50值分别为2.2和120.6 μM.WS 3在引发清凉感方面是有效的[2].
参考文献：
[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.
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