Icilin

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Chemical Structure| 36945-98-9 同义名 : AG-3-5
CAS号 : 36945-98-9
货号 : A881912
分子式 : C16H13N3O4
纯度 : 99%+
分子量 : 311.29
MDL号 : MFCD01689072
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 55 mg/mL(176.68 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

生物活性
描述 Icilin is an agonist of nonselective cation channel TRPM8, with antiproliferative activity. TRPM8 is a cation channel activated by cold temperatures and the chemical stimuli menthol and icilin[3]. The synthetic supercooling drug, icilin, and its primary receptor target, the cation channel transient receptor potential (TRP) melastatin-8 (TRPM8), have been described as potent negative regulators of inflammation in the colon. In vitro, icilin potently inhibited the proliferation of murine and human CD4+ T cells, with the peripheral expansion of autoantigen-restricted T cells similarly diminished by the administration of icilin in mice[4]. Rats injected with icilin (0.5, 1, 2.5, 5mg/kg, i.p.) displayed dose-related WDS (wet-dog shakes) that were inhibited by pretreatment with a fixed dose of clonidine (0.15 mg/kg, s.c.). alpha(2)-adrenoceptor activation inhibits shaking induced by icilin and that increases in peripheral, as well as central, alpha(2)-adrenoceptor signaling oppose the behavioral stimulant effect of icilin[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL

参考文献

[1]Lee S, Chun JN, et al. Icilin inhibits E2F1-mediated cell cycle regulatory programs in prostate cancer. Biochem Biophys Res Commun. 2013 Nov 29;441(4):1005-10.

[2]Andersson DA, Chase HW, et al. TRPM8 activation by menthol, icilin, and cold is differentially modulated by intracellular pH. J Neurosci. 2004 Jun 9;24(23):5364-9.

[3]Kühn FJ, Kühn C, Lückhoff A. Inhibition of TRPM8 by icilin distinct from desensitization induced by menthol and menthol derivatives. J Biol Chem. 2009 Feb 13;284(7):4102-11

[4]Ewanchuk BW, Allan ERO, Warren AL, Ramachandran R, Yates RM. The cooling compound icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response. FASEB J. 2018 Mar;32(3):1236-1249

[5]Kim J, Cowan A, Lisek R, Raymondi N, Rosenthal A, Hirsch DD, Rawls SM. Icilin-evoked behavioral stimulation is attenuated by alpha₂-adrenoceptor activation. Brain Res. 2011 Apr 12;1384:110-7