Overview

  • Product name

    SR-8278, REV-ERBalpha antagonist
  • Description

    REV-ERBα antagonist
  • Biological description

    REV-ERBα antagonist (EC50 = 470 nM, REV-ERBα transcriptional repression activity). Stimulates the expression of gluconeogenesis genes G6Pase and PEPCK.
  • CAS Number

    1254944-66-5
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    Ethyl 2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1H-isoquinoline-3-carboxylate
  • Molecular weight

    361.48
  • Molecular formula

    C18H19NO3S2
  • PubChem identifier

    53393127
  • Storage instructions

    Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in ethanol to 25 mM and in DMSO to 25 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CCOC(=O)C1CC2=CC=CC=C2CN1C(=O)C3=CC=C(S3)SC
  • Source

    Synthetic

  • Research areas

References

This product has been referenced in:

  • Isayama K  et al. REV-ERBa inhibits the PTGS2 expression in bovine uterus endometrium stromal and epithelial cells exposed to ovarian steroids. J Reprod Dev 60:362-70 (2014). Read more (PubMed: 25007867) »
  • Vieira E  et al. Involvement of the clock gene Rev-erb alpha in the regulation of glucagon secretion in pancreatic alpha-cells. PLoS One 8:e69939 (2013). Read more (PubMed: 23936124) »
  • Kojetin D  et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol 6:131-4 (2011). Read more (PubMed: 21043485) »

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