BMS 303141

Names

[ Name ]:
BMS 303141

[Synonym ]:
Benzenesulfonamide, 2,4-dichloro-5-hydroxy-N-(4-methoxy[1,1'-biphenyl]-2-yl)-
3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-benzenesulfonamide
BMS 303141
2,4-Dichloro-5-hydroxy-N-(4-methoxy-2-biphenylyl)benzenesulfonamide
3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide
Benzenesulfonamide, 3,5-dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-
3,5-Dichloro-2-hydroxy-N-(4-methoxy-3-biphenylyl)benzenesulfonamide
BMS-303141

Biological Activity

[Description]:

BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 of 0.13 μM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> ATP Citrate Lyase

Research Areas >> Metabolic Disease

[Target]

IC50: 0.13 uM (ACL)[1]

[In Vitro]

In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8 μM. BMS-303141 shows no cytotoxicity up to 50 lM under a cell based Alamar Blue cytotoxicity assay, indicating the observed inhibition of lipid synthesis is not a result of compound-induced cytotoxicity[1].

[In Vivo]

Chronic oral dosing of BMS-303141 in high-fat fed mice lowers approximate 20-30% plasma cholesterol and triglycerides, as well as 30-50% fasting plasma glucose. Chronic treatment with BMS-303141 shows a gradual inhibition of weight gain along with a reduction in adiposity without apparent changes in food intake. BMS-303141 shows an oral bioavailability of 55% but a relatively short half-life of 2.1 h[1].

[Animal admin]

Mice: Effect of BMS-303141 in high-fat fed mice is studied. There are a total of four groups in the study; mice on normal diet and high-fat diet controls, and two treated groups that are supplemented with BMS-303141 in their high-fat diet to an equivalent daily dose of 10 or 100 mg/kg. The study is continued for a total of 34 days. Food consumption and body weight gain are tracked along with weekly assessment of lipid and glucose plasma chemistries[1].

[References]

[1]. Li JJ, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11.

[Related Small Molecules]

SB 204990 | Furan-2-carboxylic acid

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
594.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₅Cl₂NO₄S

[ Molecular Weight ]:
424.298

[ Flash Point ]:
313.6±32.9 °C

[ Exact Mass ]:
423.009888

[ PSA ]:
84.01000

[ LogP ]:
5.39

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.653

[ Storage condition ]:
2-8℃

Safety Information

[ Hazard Statements ]:
H413

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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