SR8278

SKU: orb1940957

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 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.

Key Properties

• CAS Number: 1254944-66-5
• MW: 361.48
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉NO₃S₂
• SMILES: CCOC(=O)C1Cc2ccccc2CN1C(=O)c1ccc(SC)s1
• Target: REV-ERBα
• Solubility: DMSO:10mg/ml(27.66mM)

Bioactivity

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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

REV-ERBα