GSK-2033 | CAS#1221277-90-2 | LXR antagonist

MedKoo Cat#: 523111 | Name: GSK-2033

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK-2033 is a potent cell-active LXR antagonist (pIC50 = 7.5). It enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells and is cell permeable.

Chemical Structure

GSK-2033

CAS#1221277-90-2

Theoretical Analysis

MedKoo Cat#: 523111

Name: GSK-2033

CAS#: 1221277-90-2

Chemical Formula: C29H28F3NO5S2

Exact Mass: 591.1361

Molecular Weight: 591.66

Elemental Analysis: C, 58.87; H, 4.77; F, 9.63; N, 2.37; O, 13.52; S, 10.84

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,350.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 3,850.00	2 Weeks

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Related CAS #

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Synonym

GSK-2033; GSK2033; GSK 2033

IUPAC/Chemical Name

2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide

InChi Key

PSOXOVKYGWBTPB-UHFFFAOYSA-N

InChi Code

InChI=1S/C29H28F3NO5S2/c1-19-14-20(2)28(21(3)15-19)40(36,37)33(18-25-12-13-27(38-25)29(30,31)32)17-22-8-10-23(11-9-22)24-6-5-7-26(16-24)39(4,34)35/h5-16H,17-18H2,1-4H3

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

As shown in Fig. 1B, GSK2033 dose-dependently suppressed basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC50s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppressed the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC50s of 52 nM for LXRα and 10 nM for LXRβ (Fig. 1C). Reference: Biochem Biophys Res Commun. 2016 Oct 21;479(3):424-428. https://pubmed.ncbi.nlm.nih.gov/27680310/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMF	5.0	8.45
	DMSO	17.5	29.51

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 591.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Griffett K, Burris TP. 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. doi: 10.1016/j.bbrc.2016.09.036. Epub 2016 Sep 25. PMID: 27680310; PMCID: PMC5087326.

In vitro protocol:

In vivo protocol:

TBD

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.