CAS:1379686-30-2SR-9009

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SR9009 is an agonist of REV-ERBα and REV-ERBβ with IC50 of 670 nM and 800 nM, respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1379686-30-2

储存条件

分子式

C20H24ClN3O4S

运输

蓝冰

分子量

437.94

别名

溶解度

DMSO	250.0 mg/mL (570.9 mM)
Water	insoluble

动物实验配方

生物活性

描述The nuclear receptors REV-ERBα and -β link circadian rhythms and metabolism. SR-9009 is a potent synthetic REV-ERB agonist with IC50 value of 710nM for suppression of transcription in a cotransfection assay using full-length REV-ERB-a along with a luciferase reporter driven by the Bmal1 promoter. Administration of SR-9009 at dose of 100mg/kg, i.p., b.i.d., for 30 days resulted in a decrease in fat mass and in plasma lipids in diet-induced obese mice. SR9009 at concentration ranging in 2.5-20μM dose-dependently decreased mESC viability, rewired cellular metabolism shown by reduction of mitochondrial respiration, both of which were independent of REV-ERBs, and altered gene transcription in hepatocytes and embryonic stem cells lacking both REV-ERBα and –β, suggesting SR9009 may not be used solely as surrogate for REV-ERB activity.
作用机制SR-9009 directly binds to REV-ERB-α.^[1]
动物研究
剂量
Mice: 30 mg/kg - 100 mg/kg^[3] (i.p.)

给药途径
i.p.