LXR antagonist 2033

LXR antagonist 2033 - Names and Identifiers

Name	2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide
Synonyms	GSK 2033 LXR antagonist 2033 2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide Benzenesulfonamide, 2,4,6-trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]-
CAS	1221277-90-2

LXR antagonist 2033 - Physico-chemical Properties

Molecular Formula	C29H28F3NO5S2
Molar Mass	591.66
Solubility	Soluble in DMSO, not in water
Appearance	powder
Color	white to beige
Storage Condition	2-8°C
Use	GSK2033 is an LXR antagonist with pIC50 values of 7 and 7.4 for LXRα and LXRβ, respectively.
In vitro study	GSK2033 is a LXR antagonist with pIC 50 s 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 IC 50 s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppresses the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC 50 s of 52 nM for LXRα and 10 nM for LXRβ. GSK2033 also suppresses the expression of both of fatty acid synthase ( FASN ) and SREBP1 .
In vivo study	One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels. Plasma triglyceride levels are also unaffected by treatment with GSK2033.

LXR antagonist 2033 - Reference

Reference

1: Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p. PubMed PMID: 20345102.

LXR antagonist 2033 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	1.69 ml	8.451 ml	16.902 ml
5 mM	0.338 ml	1.69 ml	3.38 ml
10 mM	0.169 ml	0.845 ml	1.69 ml
5 mM	0.034 ml	0.169 ml	0.338 ml

Last Update：2024-01-02 23:10:35

LXR antagonist 2033 - References

biological activity	GSK2033 is an LXR antagonist, the pIC50 values for LXR α and LXR β are 7 and 7.4, respectively.
Target	pIC50: 7 (lxrα), 7.4 (lxrβ)

Last Update：2024-04-09 21:54:55