An antagonist of LXRα and LXRβ (IC50s = 0.1 and 0.398 µM

GSK2033 – 5 mg

Brand:
Cayman
CAS:
1221277-90-2
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2033 is an antagonist of liver X receptor α (LXRα) and LXRβ (IC50s = 0.1 and 0.398 µM, respectively) that has no agonist activity in an LXR transactivation assay.{36795} It inhibits LXR agonist-induced and basal expression of the LXR target genes ATP-binding cassette transporter 1 (ABCA1) and sterol regulatory element binding protein 1c (SREBP-1c) in THP-1 and HepG2 cells, respectively. However, GSK2033 binds promiscuously to a variety of nuclear receptors including RORγ, RXRα, ERα, and ERβ in a nuclear receptor specificity assay in HEK293 cells and, in a mouse model of non-alcoholic fatty liver disease (NAFLD), it induces the expression of fatty acid synthase and SREBP-1.{36796}  

 

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SKU: 25443 - 5 mg Category:

Description

An antagonist of LXRα and LXRβ (IC50s = 0.1 and 0.398 µM, respectively); inhibits LXR agonist-induced and basal expression of ABCA1 and SREBP-1c in THP-1 and HepG2 cells; binds promiscuously to a variety of nuclear receptors including RORγ, RXRα, ERα, and ERβ in a nuclear receptor specificity assay in HEK293 cells; induces the expression of fatty acid synthase and SREBP-1 in a mouse model of NAFLD

Formal name: 2,4,6-trimethyl-N-[[3′-(methylsulfonyl)[1,1′-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]-benzenesulfonamide

Synonyms: 

Molecular weight: 591.7

CAS: 1221277-90-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|FXRs & LXRs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH

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