SML0636

SR1664

≥98% (HPLC)

• Sinônimo(s): 4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid
• Fórmula empírica (Notação de Hill): C₃₃H₂₉N₃O₅
• Número CAS: 1338259-05-4
• Peso molecular: 547.60
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: powder
• condição de armazenamento: protect from light
• cor: white to beige
• solubilidade: DMSO: 15 mg/mL, clear
• temperatura de armazenamento: −20°C
• InChI: 1S/C33H29N3O5/c1-20-22(3)35(19-23-8-10-25(11-9-23)28-6-4-5-7-29(28)33(38)39)31-17-14-26(18-30(20)31)32(37)34-21(2)24-12-15-27(16-13-24)36(40)41/h4-18,21H,19H2,1-3H3,(H,34,37)(H,38,39)/t21-/m0/s1
• chave InChI: IIJDFXNUWZTHIM-NRFANRHFSA-N

Descrição

Ações bioquímicas/fisiológicas

SR1664 is a non-agonist PPARγ ligand and an inhibitor of Cdk5-mediated PPARγ phosphorylation. It has strong antidiabetic activity in two murine models of diabetes without the side effects normally asociated with the thiazolidinedione (TZD) antidiabetic PPARγ agonists. The TZD antidiabetics such as rosiglitazone and pioglitazone are full PPARγ agonists, but recent data have suggested that their separate activity, inhibition of the the obesity-linked PPARγ phosphorylation by Cdk5, is likely the more important activity for antidiabetic action. SR1664 has an IC₅₀ of 80 nM in a competitive binding assay, blocked the Cdk5-mediated phosphorylation of PPARγ in vitro with IC₅₀ between 20 and 200 nM and exhibited no PPARγ agonist activity.

Características e benefícios

This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Outras notas

Light sensitive

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable