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Merck
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SML1617

Sigma-Aldrich

GSK2033

≥98% (HPLC)

Sinonimo/i:

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

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About This Item

Formula empirica (notazione di Hill):
C29H28F3NO5S2
Numero CAS:
1221277-90-2
Peso molecolare:
591.66
Numero MDL:
MFCD28396416
Codice UNSPSC:
12352200
ID PubChem:
329825503
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 3 mg/mL, clear (warmed)

Temperatura di conservazione

2-8°C

Stringa SMILE

CS(C1=CC=CC(C2=CC=C(CN(S(C3=C(C)C=C(C)C=C3C)(=O)=O)CC4=CC=C(C(F)(F)F)O4)C=C2)=C1)(=O)=O

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
PSOXOVKYGWBTPB-UHFFFAOYSA-N

Azioni biochim/fisiol

GSK2033 has the ability to repress gluconeogenic gene expression stimulated by GC (glucocorticoids), without altering immune-responsive GR (GC receptor) target genes. It helps to target several nuclear receptors that can alter hepatic gene expression.
GSK2033 is an antagonist of the nuclear receptor liver-X-receptor (LXR) with pIC50 values of 7.0 for LXRα and 7.4 for LXRβ. Treatment of murine CD41 T cells with GSK2033 enhanced cellular proliferation and Th1/Th2/Th17 differentiation. In another study, the conjugated linoleic acid (CLA)-induced expression of efflux protein ATP-binding-cassette transporter A1 (ABCA1) was completely abolished by preincubation with GSK2033, showing that CLA mediated regulation of ABCA-1 expression is LXR dependent.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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Separating the Anti-Inflammatory and Diabetogenic Effects of Glucocorticoids Through LXRβ Antagonism.
Patel R, et al.
Endocrinology, 158(4), 1034-1047 (2017)
Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease.
Griffett K and Burris TP
Biochemical and Biophysical Research Communications, 479(3), 424-428 (2016)
Lili Chen et al.
Journal of neurochemistry, 154(2), 205-217 (2019-10-12)
Cerebral ischemia (CI) leads to cognitive dysfunction due to the loss of hippocampal neurons. Liver X receptors (LXRs), including the LXRα and LXRβ isoforms, are critical for neurogenesis, synaptic plasticity, neurodegeneration, and cholesterol metabolism. However, the potential role of LXRs
Louise Ménégaut et al.
Cell reports, 31(7), 107665-107665 (2020-05-21)
Low-grade inflammation is constitutive of atherosclerosis, and anti-inflammatory therapy inhibiting interleukin-1β (IL-1β) reduces the rate of cardiovascular events. While cholesterol accumulation in atheroma plaque and macrophages is a major driver of the inflammatory process, the role of the LXR cholesterol

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