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CAS No.: 1254944-66-5

SR8278 Catalog No. CSN23132

SR8278 is a rev-erbα antagonist. It inhibits Rev-Erbα transcriptional repression (EC50 = 0.47 μM) and blocks activity of Rev-Erbα agonist GSK 4112 in HEK293 cells. SR8278 increases expression of glucose-regulating genes, G6Pase and PEPCK in HepG2 cells.

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技术信息

生物活性

描述REV-ERBα is a member of the nuclear receptor superfamily that functions as a receptor for the porphoryin heme. REV-ERBα suppresses transcription of its target genes in a heme-dependent manner. SR8278 displays REV-ERBα antagonist activity in contrast to the agonist activity displayed by GSK4112. Addition of SR8278 shows the opposite effect enhancing the expression of the reporter gene presumably due to blocking the action of the endogenous agonist heme. Addition of the antagonist, SR8278, results in inhibition of the REV-ERBα transcriptional repression activity in a dose-dependent manner (EC₅₀=0.47μM). Treatment of HepG2 cells with 10 μM SR8278 for 24 h resulted in a significant increase in the expression of REV-ERBα target genes consistent with the compound blocking the action of the endogenous agonist, heme^[1]. Specifically, the values of areas under plasma concentration time curves (AUC), initial plasma concentrations (C₀), elimination half-lives (t_1/2), and clearances (CL) were 608.33 ± 295.25 vs. 598.59 ± 276.92 ng·h/mL, 2410.25 ± 202.36 vs. 3742.11 ± 1300.21 ng/mL, 0.17 ± 0.08 vs. 0.11 ± 0.04 h, 3330.83 ± 1609.48 vs. 3364.81 ± 1111.38 mL/kg·h for SR8278 in normal rats vs. diabetic rats, respectively^[2].
参考文献

[1] Kojetin D, Wang Y, Kamenecka TM, Burris TP. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol. 2011;6(2):131‐134
[2] Dong D, Sun H, Wu Z, Wu B, Xue Y, Li Z. A validated ultra-performance liquid chromatography-tandem mass spectrometry method to identify the pharmacokinetics of SR8278 in normal and streptozotocin-induced diabetic rats. J Chromatogr B Analyt Technol Biomed Life Sci. 2016;1020:142‐147

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7664 mL
- 13.8321 mL
- 27.6642 mL
- 5 mM
- 0.5533 mL
- 2.7664 mL
- 5.5328 mL
- 10 mM
- 0.2766 mL
- 1.3832 mL
- 2.7664 mL

技术信息

CAS号

1254944-66-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H19NO3S2

运输

蓝冰

分子量

361.48

别名

溶解度

DMSO	95.0 mg/mL (262.8 mM) warming

动物实验配方

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SR8278 Catalog No. CSN23132

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