| Description | SR8278 is an REV-ERBα antagonist(EC50 = 0.47 μM), blocking activation of the receptor by the synthetic agonist GSK 4112 |
| In vitro | SR8278刺激肝细胞中两个REV-ERBα目标基因的表达，这两个基因参与调节葡萄糖产生，即葡萄糖-6-磷酸酶和磷酸烯醇丙酮酸羧激酶[1]。 |
| molecular weight | 361.48 |
| Molecular formula | C18H19NO3S2 |
| CAS | 1254944-66-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (138.32 mM,）, Sonication is recommended. |
| References | 1. Kojetin D , Wang Y , Kamenecka T M , et al. Identification of SR8278, a Synthetic Antagonist of the Nuclear Heme Receptor REV-ERB[J]. Acs Chemical Biology, 2011, 6(2):131-134. 2. Dong D , Sun H , Wu Z , et al. A validated ultra-performance liquid chromatography-tandem mass spectrometry method to identify the pharmacokinetics of SR8278 in normal and streptozotocin-induced diabetic rats[J]. Journal of Chromatography B, 2016, 1020:142-147. |
| Citations | 1. Zhong D, Chen J, Qiao R, et al.Genetic or pharmacologic blockade of mPGES-2 attenuates renal lipotoxicity and diabetic kidney disease by targeting Rev-Erbα/FABP5 signaling.Cell Reports.2024, 43(4). |