5.30351

Nrf2 Activator IV, VSC2

• Sinônimo(s): Nrf2 Activator IV, VSC2, ( E)-1-Chloro-2-(2-(2-methoxyphenylsulfonyl)vinyl)benzene, Nuclear Factor E2-related Factor 2 Activator IV, VSC2, (E)-1-Chloro-2-(2-(2-methoxyphenylsulfonyl)vinyl)benzene, Nuclear Factor E2-related Factor 2 Activator IV, VSC2
• Fórmula empírica (Notação de Hill): C₁₅H₁₃ClO₃S
• Número CAS: 1554271-18-9
• Peso molecular: 308.78
• Número MDL: MFCD31800430
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: off-white
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

A cell-permeable vinylsulfone compound that acts as a more potent Nrf-2 activator than the analogous α,β-unsaturated ketone-based chalcones (e.g. Cat. No. 492040 ) in stimulating HO-1 expression in murine microglial BV-2 cultures (382% of control protein level in 24 h; 20 µM). Drug treatment in murine dopaminergic (DAergic) CATH.a cultures likewise effectively induces Nrf2 nuclear translocation (Fold of control in 3 h/dose = 1.4/1 µM, 2.3/5 µM, 3.4/10 µM) and overall Nrf2 cellular accumulation (Fold of control in 24 h/dose = 1.5/0.5 µM, 2.0/1 µM, 2.8/2 µM, 4.3/5 µM), presumably by freeing Nrf2 from its negative regulator keap1, with concomitant upregulation of Nrf2-regulated antioxidant enzymes expression, including heme oxygenase-1/OH-1, NAD(P)H quinone oxidoreductase 1/NQO1, glutamate-cysteine ligase modifier & catalytic subunits, QCLM & GCLC. Shown to protect CATH.a against BH4 toxicity (effective conc. 0.1 to 1.0 µM against 200 µM BH4 for 24 h) in vitro and prevent MPTP- (Cat. No. 506382 ) induced motor deficits/dysfunctions (by vertical grid test 6 d post MPTP injection) and neurodegeneration (by TH staining 7 d post MPTP injection) in a murine PD model in vivo (3 X 10 mg drug/kg/d oral dosages; 4X 20 mg MPTP/kg/2 h i.p. dosages starting 24 h post the 1st drug dosage).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Use only fresh DMSO for reconstitution.

Outras notas

Lee, J.A., et al. 2015. Br. J. Pharmacol.172, 1087.
Woo, S.Y., et al. 2014. J. Med. Chem.57, 1473.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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