1221277-90-2
1221277-90-2 structure
- Name: GSK 2033
- Chemical Name: 2,4,6-Trimethyl-N-{[3'-(methylsulfonyl)-4-biphenylyl]methyl}-N-{[5-(trifluoromethyl)-2-furyl]methyl}benzenesulfonamide
- CAS Number: 1221277-90-2
- Molecular Formula: C29H28F3NO5S2
- Molecular Weight: 591.661
- Catalog: Signaling Pathways Metabolic Enzyme/Protease LXR
- Create Date: 2018-03-26 05:11:04
- Modify Date: 2024-01-08 16:25:58
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GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
| Name | 2,4,6-Trimethyl-N-{[3'-(methylsulfonyl)-4-biphenylyl]methyl}-N-{[5-(trifluoromethyl)-2-furyl]methyl}benzenesulfonamide |
|---|---|
| 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 |
| 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 |
| 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℃ |