GSK3987

CAS No. 264206-85-1

GSK3987( )

Catalog No. M27880 CAS No. 264206-85-1

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 230 Get Quote
10MG 372 Get Quote
25MG 623 Get Quote
50MG 887 Get Quote
100MG 1197 Get Quote
500MG 2394 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    GSK3987
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.
  • Description
    GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.(In Vitro):In primary human macrophages, GSK3987 (30, 100, 300, 1000 nM) increased the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner. In human hepatoma (HepG2) cells, GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in a dose-dependent manner. GSK3987 showed activity with EC50s of 0.08 μM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively.
  • In Vitro
    RT-PCR Cell Line:HepG2 cells Concentration:6-1500 nM Incubation Time:Result:Increased the expression of SREBP-1c and induced triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner.
  • In Vivo
  • Synonyms
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    EP4
  • Research Area
  • Indication

Chemical Information

  • CAS Number
    264206-85-1
  • Formula Weight
    384.435
  • Molecular Formula
    C24H20N2O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (260.13 mM)
  • SMILES
    COc1ccc(NC2=C(C(=O)N(Cc3ccccc3)C2=O)c2ccccc2)cc1
  • Chemical Name

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Yang JJ,?et al. Discovery and Characterization of 1H-1,2,3-Triazole Derivatives as Novel Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy. J Med Chem.?2020 Jan 23;63(2):569-590.
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