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GSK 2033

Names

[ CAS No. ]:
1221277-90-2

[ Name ]:
GSK 2033

[Synonym ]:
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

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> LXR
Research Areas >> Metabolic Disease

[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.


[Related Small Molecules]

T0901317 | GW3965 HCl | WAY 252623 | SR 9243 | (20S)-Protopanaxatriol | 27-Hydroxycholesterol | AZ876 | SR 9238 | 24-Hydroxycholesterol | BMS-779788 | BMS-852927 | Nagilactone B | RGX-104 | Rovazolac

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℃

Related Compounds