GSK3987

GSK3987 is a dual agonist of liver X receptor alpha (LXRalpha) and LXRbeta. It recruits steroid receptor coactivator 1 (SRC-1) to LXRalpha and LXRbeta in a ligand-sensing assay (LiSA, EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXRalpha and LXRbeta over a panel of nuclear receptors and GSK3beta (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.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: (Request formulation change), A solid. Solubility: DMSO: 200 mg/ml, Methanol: 100 mg/ml. lambdamax: 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.