SML2829
SB-204990
≥98% (HPLC), ATP citrate-lyase inhibitor, powder
别名:
(+/-) (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
产品名称
SB-204990, ≥98% (HPLC)
SMILES string
Clc1c(ccc(c1)Cl)CCCCCC[C@H]2OC(=O)[C@@](C2)(O)CC(=O)O
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
InChI key
YTRNLFYTHYWDAU-KDOFPFPSSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
ATP citrate-lyase inhibitor SB-201076 γ-lactone prodrug with cell-permeability, oral availability and in vivo hypocholesterolaemic/hypolipidaemic efficacy.
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).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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
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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