5.30351

Nrf2 Activator IV, VSC2

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₅H₁₃ClO₃S
• CAS-Nummer: 1554271-18-9
• Molekulargewicht: 308.78
• MDL-Nummer: MFCD31800430
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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).

Biochem./physiol. Wirkung

Cell permeable: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Use only fresh DMSO for reconstitution.

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable