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Merck
모든 사진(1)

Key Documents

SML2829

Sigma-Aldrich

SB-204990

≥98% (HPLC)

동의어(들):

(+/-) (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

실험식(Hill 표기법):
C18H22Cl2O5
CAS Number:
Molecular Weight:
389.27
UNSPSC 코드:
51111800
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

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

InChI key

YTRNLFYTHYWDAU-KDOFPFPSSA-N

생화학적/생리학적 작용

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).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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

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