G5547

GSK837149A

≥98% (HPLC), solid

• Sinônimo(s): N,N′-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea
• Fórmula empírica (Notação de Hill): C₂₃H₂₂N₈O₅S₂
• Número CAS: 13616-29-0
• Peso molecular: 554.60
• Código UNSPSC: 51111800
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• cor: white to off-white
• solubilidade: DMSO: >10 mg/mL; H₂O: insoluble
• originador: GlaxoSmithKline
• temperatura de armazenamento: 2-8°C

Descrição

Ações bioquímicas/fisiológicas

GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors.

Características e benefícios

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Informações de segurança

• Pictogramas: GHS07
• Palavra indicadora: Warning
• Frases de perigo: H319
• Declarações de precaução: P264 - P280 - P305 + P351 + P338 - P337 + P313
• Classificações de perigo: Eye Irrit. 2
• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable
• Equipamento de proteção individual: dust mask type N95 (US), Eyeshields, Gloves