Product Name :
GSK2033
Description:
GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
CAS:
1221277-90-2
Molecular Weight:
591.66
Formula:
C29H28F3NO5S2
Chemical Name:
N-(3′-methanesulfonyl-[1,1′-biphenyl]-4-ylmethyl)-2,4,6-trimethyl-N-[5-(trifluoromethyl)furan-2-yl]methylbenzene-1-sulfonamide
Smiles :
CS(=O)(=O)C1=CC(=CC=C1)C1C=CC(CN(CC2=CC=C(O2)C(F)(F)F)S(=O)(=O)C2C(C)=CC(C)=CC=2C)=CC=1
InChiKey:
PSOXOVKYGWBTPB-UHFFFAOYSA-N
InChi :
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
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.|Product information|CAS Number: 1221277-90-2|Molecular Weight: 591.66|Formula: C29H28F3NO5S2|Chemical Name: N-(3′-methanesulfonyl-[1,1′-biphenyl]-4-ylmethyl)-2,4,6-trimethyl-N-[5-(trifluoromethyl)furan-2-yl]methylbenzene-1-sulfonamide|Smiles: CS(=O)(=O)C1=CC(=CC=C1)C1C=CC(CN(CC2=CC=C(O2)C(F)(F)F)S(=O)(=O)C2C(C)=CC(C)=CC=2C)=CC=1|InChiKey: PSOXOVKYGWBTPB-UHFFFAOYSA-N|InChi: 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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 30 mg/mL (50.NAD+/NADH Assay Kit Epigenetics 70 mM; Need ultrasonic and warming).ARRY-382 Protein Tyrosine Kinase/RTK |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.PMID:32310431 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.|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.|References:|Zuercher WJ, et al. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6.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.Products are for research use only. Not for human use.|
