A dual agonist of LXRα and LXRβ
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GSK3987

Item No. 30954

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione
CAS Number
264206-85-1
Molecular Formula
C24H20N2O3
Formula Weight
384.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 200 mg/mlMethanol: 100 mg/ml
λmax
242 nm
SMILES
O=C(N1CC2=CC=CC=C2)C(C3=CC=CC=C3)=C(NC4=CC=C(OC)C=C4)C1=O
InChi Code
InChI=1S/C24H20N2O3/c1-29-20-14-12-19(13-15-20)25-22-21(18-10-6-3-7-11-18)23(27)26(24(22)28)16-17-8-4-2-5-9-17/h2-15,25H,16H2,1H3
InChi Key
HLZMYWLMBBLASX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $432

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    Product Description

    GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.1 It recruits steroid receptor coactivator 1 (SRC-1) to LXRα and LXRβ in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXRα and LXRβ over a panel of nuclear receptors and GSK3β (IC50 = >5,000 nM) but does induce ABCA1 expression in a reporter assay using THP-1 cells (EC50 = 80 nM). It inhibits LPS-induced IL-6 secretion in THP-1 macrophages. GSK3987 increases the expression of the sterol regulatory element binding protein 1c (SREBP-1c) and induces triglyceride accumulation in HepG2 cells in a concentration-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jaye, M.C., Krawiec, J.A., Campobasso, N., et al. Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. J. Med. Chem. 48(17), 5419-5422 (2005).