1. Metabolic Enzyme/Protease
  2. LXR

GSK2033 

Cat. No.: HY-108688 Purity: 98.83%
Handling Instructions

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

For research use only. We do not sell to patients.

GSK2033 Chemical Structure

GSK2033 Chemical Structure

CAS No. : 1221277-90-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 156 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 756 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (50.70 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6902 mL 8.4508 mL 16.9016 mL
5 mM 0.3380 mL 1.6902 mL 3.3803 mL
10 mM 0.1690 mL 0.8451 mL 1.6902 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

591.66

Formula

C₂₉H₂₈F₃NO₅S₂

CAS No.

1221277-90-2

SMILES

O=S(C1=C(C)C=C(C)C=C1C)(N(CC2=CC=C(C3=CC=CC(S(=O)(C)=O)=C3)C=C2)CC4=CC=C(C(F)(F)F)O4)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GSK2033
Cat. No.:
HY-108688
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GSK2033

Cat. No.: HY-108688