| Identification | Back Directory | [Name]
SB 204990 | [CAS]
154566-12-8 | [Synonyms]
SB 204990
YTRNLFYTHYWDAU-KDOFPFPSSA-N
(3R,5S)-rel-5-[6-(2,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid
2-((3R,5S)-5-(6-(2,4-dichlorophenyl)hexyl)-3-hydroxy-2-oxotetrahydrofuran-3-yl)acetic acid
3-Furanacetic acid, 5-[6-(2,4-dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-, (3R,5S)-rel- | [Molecular Formula]
C18H22Cl2O5 | [MOL File]
154566-12-8.mol | [Molecular Weight]
389.27 |
| Chemical Properties | Back Directory | [Melting point ]
87-89 °C | [Boiling point ]
571.6±40.0 °C(Predicted) | [density ]
1.332±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMF: 30 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 20 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
4.33±0.10(Predicted) | [color ]
White to off-white | [InChI]
InChI=1/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+/s3 | [InChIKey]
YTRNLFYTHYWDAU-RVFWCEGZNA-N | [SMILES]
O1[C@@H](CCCCCCC2=CC=C(Cl)C=C2Cl)C[C@@](O)(CC(O)=O)C1=O |&1:1,17,r| |
| Hazard Information | Back Directory | [Uses]
SB 204990 is a prodrug of the potent ATP citrate-lyase inhibitor SB-201076. | [Biological Activity]
SB-204990 is a cell-permeable and orally available γ-lactone prodrug of the non-cell-permeable SB-201076 th at inhibits human and r at ATP citrate-lyase (Ki =1 μM against human and r at 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%respectivelywith 30 μM SB-204990)and display hypocholesterolaemic and hypolipidaemic efficacy in vivo when administered in the diet (0.05-0.25%w/w; miceratsdogs). | [in vivo]
SB 204990, when administered orally to rats, is absorbed into the systemic circulation. When administered in the diet (0.05-0.25%, w/w) for 1 week, SB 204990 causes a dose-related decrease in plasma cholesterol (by up to 46%) and triglyceride levels (by up to 80%) in rats. SB 204990 (25 mg/kg per day) also decreases plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels[2]. | [storage]
Store at -20°C |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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