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Merck
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Documenti

SML2829

Sigma-Aldrich

SB-204990

≥98% (HPLC)

Sinonimo/i:

(+/-) (3R*,5S*)-rel-5-[6-(2,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid, SB 201076 prodrug, SB 204990, SB-201076 prodrug, SB201076 prodrug, SB204990

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About This Item

Formula empirica (notazione di Hill):
C18H22Cl2O5
Numero CAS:
154566-12-8
Peso molecolare:
389.27
Codice UNSPSC:
51111800
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

InChI

1S/C18H22Cl2O5/c19-13-8-7-12(15(20)9-13)5-3-1-2-4-6-14-10-18(24,11-16(21)22)17(23)25-14/h7-9,14,24H,1-6,10-11H2,(H,21,22)/t14-,18+/m1/s1
YTRNLFYTHYWDAU-KDOFPFPSSA-N

Azioni biochim/fisiol

SB-204990 is a cell-permeable and orally available γ-lactone prodrug of the non-cell-permeable SB-201076 that inhibits human and rat ATP citrate-lyase (Ki =1 μM against human and rat ACL) in a predominantly competitive manner with a small but significant uncompetitive component. SB-204990 treatment is shown to suppress the rate of cellular cholesterol and fatty acid synthesis in HepG2 cultures (by 91% & 82%, respectively, with 30 μM SB-204990), and display hypocholesterolaemic and hypolipidaemic efficacy in vivo when administered in the diet (0.05-0.25%, w/w; mice, rats, dogs).

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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N J Pearce et al.
The Biochemical journal, 334 ( Pt 1), 113-119 (1998-08-07)
ATP citrate (pro-S)-lyase (EC 4.1.3.8), a cytosolic enzyme that generates acetyl-CoA for cholesterol and fatty acid synthesis de novo, is a potential target for hypolipidaemic intervention. Here we describe the biological effects of the inhibition of ATP citrate-lyase on lipid
B J van Vlijmen et al.
Arzneimittel-Forschung, 48(4), 396-402 (1998-06-03)
Apolipoprotein (APO) E*3-Leiden mice with impaired chylomicron and VLDL (very low density lipoprotein) remnant metabolism display hyperlipidaemia and atherosclerosis. In the present study, these mice were used for testing the hypolipidaemic effect of two marketed agents, lovastatin (CAS 75330-75-5) and
Brianna H Shares et al.
The Journal of biological chemistry, 293(41), 16019-16027 (2018-08-29)
Bone marrow stromal (a.k.a. mesenchymal stem) cells (BMSCs) can differentiate into osteoblasts (OBs), adipocytes, or chondrocytes. As BMSCs undergo OB differentiation, they up-regulate mitochondrial oxidative phosphorylation (OxPhos). Here, we investigated the mechanism(s) connecting mitochondrial OxPhos to OB differentiation. First, we
Federico Pietrocola et al.
Cancer cell, 30(1), 147-160 (2016-07-15)
Caloric restriction mimetics (CRMs) mimic the biochemical effects of nutrient deprivation by reducing lysine acetylation of cellular proteins, thus triggering autophagy. Treatment with the CRM hydroxycitrate, an inhibitor of ATP citrate lyase, induced the depletion of regulatory T cells (which dampen
Glenn R Bantug et al.
Immunity, 48(3), 542-555 (2018-03-11)
Glycolysis is linked to the rapid response of memory CD8+ T cells, but the molecular and subcellular structural elements enabling enhanced glucose metabolism in nascent activated memory CD8+ T cells are unknown. We found that rapid activation of protein kinase B (PKB
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