GSK 2033

Modify Date: 2024-01-08 16:25:58

GSK 2033 Structure
GSK 2033 structure
Common Name GSK 2033
CAS Number 1221277-90-2 Molecular Weight 591.661
Density 1.3±0.1 g/cm3 Boiling Point 734.7±70.0 °C at 760 mmHg
Molecular Formula C29H28F3NO5S2 Melting Point N/A
MSDS N/A Flash Point 398.1±35.7 °C

 Use of GSK 2033


GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.

 Names

Name 2,4,6-Trimethyl-N-{[3'-(methylsulfonyl)-4-biphenylyl]methyl}-N-{[5-(trifluoromethyl)-2-furyl]methyl}benzenesulfonamide
Synonym More Synonyms

 GSK 2033 Biological Activity

Description GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
Related Catalog
Target

pIC50: 7 (LXRα), 7.4 (LXRβ)[1]

In Vitro GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively. GSK2033 dose-dependently suppresses basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC50s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppresses the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC50s of 52 nM for LXRα and 10 nM for LXRβ. GSK2033 also suppresses the expression of both of fatty acid synthase (FASN) and SREBP1[2].
In Vivo One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels. Plasma triglyceride levels are also unaffected by treatment with GSK2033[2].
Cell Assay HepG2 cells are maintained in minimal essential medium supplemented with 10% FBS and antibiotics. HepG2 cells are then treated for 24 h with GSK2033 followed by assessment of expression of genes by qPCR[2].
Animal Admin 21-week old male C57BL6 DIO mice are used. Animals are individually housed and fed a high fat diet (60% kcal/fat diet, 20% carbohydrate) for the duration of the experiment that includes GSK2033 administration for 28 days (30 mg/kg, q. d, i. p.). Body weight and food intake are monitored daily[2].
References

[1]. Zuercher WJ, et al. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6.

[2]. Griffett K, et al. Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease. Biochem Biophys Res Commun. 2016 Oct 21;479(3):424-428.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 734.7±70.0 °C at 760 mmHg
Molecular Formula C29H28F3NO5S2
Molecular Weight 591.661
Flash Point 398.1±35.7 °C
Exact Mass 591.136108
LogP 6.62
Vapour Pressure 0.0±2.4 mmHg at 25°C
Index of Refraction 1.572
Storage condition 2-8℃

 Synonyms

2,4,6-Trimethyl-N-{[3'-(methylsulfonyl)-4-biphenylyl]methyl}-N-{[5-(trifluoromethyl)-2-furyl]methyl}benzenesulfonamide
Benzenesulfonamide, 2,4,6-trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]-
GSK2033
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