SR8278

Research use only, not for human use.

SR8278 is an REV-ERBα antagonist(EC50 = 0.47 μM) blocking activation of the receptor by the synthetic agonist GSK 4112.

SR8278 is an REV-ERBα antagonist(EC50 = 0.47 μM) blocking activation of the receptor by the synthetic agonist GSK 4112.(In Vitro):SR8278 has REV-ERBα transcriptional repression inhibitory activity with an EC50 of 0.47μM.(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.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.

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

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.

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Others

Other Targets

REV-ERBα

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1254944-66-5

361.48

C18H19NO3S2

>98% (HPLC)

DMSO:10mg/ml(27.66mM)

CCOC(=O)C1Cc2ccccc2CN1C(=O)c1ccc(SC)s1

ethyl 2-{[5-(methylsulfanyl)thiophen-2-yl]carbonyl}-1234-tetrahydroisoquinoline-3-carboxylate

(-20℃)

With Ice Pack

≥ 2 years