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SR9009

CAS No. : 1379686-30-2

MCE 站：SR9009

产品活性：SR9009 是 REV-ERBα/β 激动剂，作用 REV-ERBα 和 REV-ERBβ 的 IC₅₀ 分别为 670 nM 和 800 nM。

研究领域：Autophagy

作用靶点：Autophagy

In Vitro: SR9009 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD)-REV-ERB ligand binding domain (LBD)α or β ａnd a Gal4-responsive luciferase reporter (SR9009: REV-ERBα IC₅₀=670 nM, REV-ERBβ IC₅₀=800 nM). SR9009 potently ａnd efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (IC₅₀=710 nM). SR9009 suppresses the expression of BMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner. Direct binding of the SR9009 to REV-ERBα is also confirmed using circular dichrosim analysis (K_d=800 nM).

In Vivo: While the stress of handling ａnd twice-daily injections caused weight loss in vehicle-treated controls, weight loss of SR9009-treated animals is 60% greater. SR9009 (100 mg/kg ,i.p.) treated mice exhibit a more severe reduction in adiposity. Plasma non-esterified fatty acids (NEFA) are also reduced (23%) along with plasma glucose (19%) in the SR9009 treated animals. In the white adipose tissue (WAT) , SR9009 treatment results in a decrease in expression of genes encoding enzymes involved in triglyceride (TG) synthesis as is also observed in lean mice.

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