Product Description

Sarms SR9011
CAS : 1379686-30-2
Purity:99% HPLC
Packing:10g,100g,500g and 1kg
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Benefit：SR9011 suppressed the expression of BMAL1 messenger RNA in HepG2 cells in a REV-ERB-a/b-dependent manner. Moreover, SR9011 inhibited the activity of the SCNclock, with reversible inhibition of circadian oscillations.
The C-terminal of sr9011 family proteins lacks a ligand binding domain, but the expression of Rev Erb protein can be inhibited by recruiting nuclear receptor inhibitors and histone deacetylase 3. Histone deacetylase 3 is a rev Erb agonist and a small molecular chemical probe. Fon Taine et al. First reported that sr9011 has a correlation with inflammation, sr9011 can inhibit the expression of TR4, thus controlling the inflammatory signal. Foreign scholars have found that in human macrophages, the increase of sr9011 mRNA expression by pharmacological methods directly leads to the decrease of pro-inflammatory factor IL-6 mRNA expression.
Sr9011 increased the expression of chimeric Gal4 DNA binding domain in HEK293 cells in a dose-dependent manner to evaluate Rev Erb dependent inhibitory activity (DBD) - Rev Erb ligand binding domain (LBD) α or β and Gal4 responsive luciferase (Rev Erb α IC50 = 790 nm, Rev Erb β IC50 = 560 nm).

Sr9011 can effectively inhibit the luciferase reporter gene transcription (sr9011 IC50 = 620 nm) driven by BMAL1 promoter with full-length Rev Erb α in CO transfection experiment. Sr9011 inhibits mRNA expression of ofbmal1 in Rev Erb α / β dependent [1] sr9011 inhibits the proliferation of breast cancer cells in HepG2 cells,
Regardless of ER and HER2 status. Sr9011 seems to pause the cell cycle of breast cancer cells before the M phase. Cyclin A (ccna2) was identified as a direct target gene of Rev Erb, indicating that sr9011, which inhibits the expression of this cyclin, may mediate cell cycle arrest. Zhiliao sr9011 increased the number of cells in G0 / G1 phase, decreased the number of cells in S phase and G2 / M phase, indicating that activated Rev Erb may decrease the number of cells in G1 to S phase transition phase and / or from s to G2 / M phase [2].
Sr9011 is a rev Erb agonist. Rev Erb α and rev Erb β are regulated by IC50 at 790 nm and 560 nm, respectively. Sr9011 is not active in other nuclear receptors. The clock of SCN activity in SR 9011 block was reversibly inhibited by per2 Luc. The expression of several metabolic genes in liver, skeletal muscle and adipose tissue in the circadian pattern could also be changed in SR 9011 mice, resulting in increased energy consumption.
Sr9011 is a rev Erb - α / β agonist. The role of nuclear Erb oscillators in the regulation of circadian rhythms. Both BMAL1 and clock are direct targets of Rev Erb. The loss of Rev Erb - α alters circadian rhythm.

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