| Bioactivity | SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease[1][2][3]. | ||||||||||||
| Target | EC50: 0.47 μM (REV-ERBα). | ||||||||||||
| Invitro | SR8278 has REV-ERBα transcriptional repression inhibitory activity with an EC50 of 0.47μM[1]. | ||||||||||||
| In Vivo | SR8278 (slow microinjection; 20 μg/mouse) exerts antidepressant and anxiolytic effects in a circadian time-dependent manner in 6-OHDA-lesioned mice and restores the circadian rhythm of mood-related behaviors[1]. SR8278 (slow microinjection; 20 μg/mouse) restores the binding activities of REV-ERBα and NURR1 to the tyrosine hydroxylase promoter and the induction of enrichment of the R/N motif, recognized by REV-ERBα and NURR1[1]. Animal Model: | ||||||||||||
| Name | SR8278 | ||||||||||||
| CAS | 1254944-66-5 | ||||||||||||
| Formula | C18H19NO3S2 | ||||||||||||
| Molar Mass | 361.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kojetin , et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol. 2011 Feb 18;6(2):131-4. [2]. Dong D, 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 Chromatogr B Analyt Technol Biomed Life Sci. 2016 May 1;102 [3]. Jeongah Kim, et al. Pharmacological Rescue with SR8278, a Circadian Nuclear Receptor REV-ERBα Antagonist as a Therapy for Mood Disorders in Parkinson's Disease. Neurotherapeutics. 2022 Mar;19(2):592-607. |