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SR8278

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Chemical Structure| 1254944-66-5 同义名 : -
CAS号 : 1254944-66-5
货号 : A915123
分子式 : C18H19NO3S2
纯度 : 99%+
分子量 : 361.478
MDL号 : MFCD18782736
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(290.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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 (t1/2), 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.83mL

2.77mL

1.38mL

27.66mL

5.53mL

2.77mL
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