货号	规格	价格	上海	北京	珠海	重庆	武汉
S87967-5mg买3赠1	99.40%	￥240.00 S87967-5mg ￥240.00 现货（买3赠1）	5 5	-	-	-	-
S87967-10mg买3赠1	99.40%	￥335.00 S87967-10mg ￥335.00 现货（买3赠1）	3 3	-	-	-	-
S87967-25mg买3赠1	99.40%	￥580.00 S87967-25mg ￥580.00 现货（买3赠1）	5 5	-	-	-	-
S87967-50mg买3赠1	99.40%	￥960.00 S87967-50mg ￥960.00 现货（买3赠1）	4 4	-	-	-	-
S87967-100mg买3赠1	99.40%	￥1800.00 S87967-100mg ￥1800.00 现货（买3赠1）	5 5	-	-	-	-

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产品描述：

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

靶点：

EC50: 0.47 μM (REV-ERBα)

体外研究：

SR8278 has REV-ERBα transcriptional repression inhibitory activity with an EC50 of 0.47μM

体内研究：

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. 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. Animal Model: 6-OHDA-lesioned mice Dosage: 20 μg/mouse Administration: slow microinjection; 20 μg/mouse Result: Recovered mood-related behavioral deficits shown in 6-OHDA-lesioned mice.Altered remaining DAergic neuron specific transcription levels of REV-ERBα and Nurr1 in the VTA.Restored antagonistic crosstalk of REV-ERBα and NURR1 binding activity to TH promoter and TH protein levels in VTA.Induced enrichments of REV-ERBα and NURR1 binding motifs at dawn.

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.766 ml	13.832 ml	27.664 ml
5 mM	0.553 ml	2.766 ml	5.533 ml
10 mM	0.277 ml	1.383 ml	2.766 ml
50 mM	0.055 ml	0.277 ml	0.553 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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SR 8278