CAS:1254205-52-1RQ-00203078

RQ-00203078 is a selective antagonist of TRPM8 with IC50 of 8.3 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1254205-52-1

储存条件

分子式

C21H13ClF6N2O5S

运输

蓝冰

分子量

554.85

别名

溶解度

DMSO	155.0 mg/mL (279.4 mM)
Water	insoluble

动物实验配方

生物活性

描述TRPM8 is a Ca²⁺- permeable, nonselective cation channel, expressed on primary sensory neurons. TRPM8 is activated by cold temperature in both the innocuous (15-28ºC) and noxious (<15ºC) range, as well as by chemical agonists such as menthol and icilin 1, thus making it play a role in cold hyperalgesia and cold allodynia induced by disease conditions. RQ-00203078 is a highly selectvie and potent TRPM8 antagonist with IC50 value of 8.3nM for inhibition of menthol (30μM) induced Ca2+ influx in HEK293 cells. Oral administration of RQ-00203078 at doses of 0.3, 1, 3 and 10 mg/kg 1hour prior to icilin injection to fasted rats dose-dependently attenuated the icilin-induced wet-dog shaking behavior. Treatment with 10μM RQ-00203078 attenuated TRPM8-mediated effects on cell-motility at 12h post treatment, and reduced cell invasion activity at 22h post treatment in HSC cell lines. Meanwhile, RQ-00203078 at 10μM suppressed the MMP-9 activity seen in the presence of menthol (100μM) post 24-hour treatment.
动物研究
剂量
Rat: 1 mg/kg - 10 mg/kg^[2] (p.o.); 0.1 mg/kg - 3 mg/kg^[3] (i.v.); 3 mg/kg^[4] (I.p.)

给药途径
p.o., i.v., i.p.

动物研究
剂量	Rat: 1 mg/kg - 10 mg/kg^[2] (p.o.); 0.1 mg/kg - 3 mg/kg^[3] (i.v.); 3 mg/kg^[4] (I.p.)
给药途径	p.o., i.v., i.p.