SML2819

AZ12799734

≥98% (HPLC)

• Synonym(e): 4-[[4-[(2,6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide, 4-[[4-[(2,6-Dimethylpyridin-3-yl)oxy]pyridin-2-yl]amino]benzenesulfonamide, AZ 12799734, AZ-12799734
• Empirische Formel (Hill-System): C₁₈H₁₈N₄O₃S
• CAS-Nummer: 1117684-36-2
• Molekulargewicht: 370.43
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Beschreibung

Biochem/physiol Actions

AZ12799734 is an orally active TGF-β type I receptors active site inhibitor (ALK1/2/3/4/5/6 K_d = 7.1/6.2/40/1/0.74/0.017 μM) that inhibits ALK5-dependent Smad2 nuclear translocation upon TGF-β1 stimulation (IC₅₀ = 17 nM; MDA-MB-468), as well as ALK1/2/3/6-mediated Smad1 and ALK4/5/7-mediated Smad2 phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12799734 oral administration in rats results in heart valve lesions (200 mg/kg/day for 5 days) and physeal dysplasia (400 mg/kg/day for 6 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.

Orally active TGF-β type I receptors ALK1-7 active site inhibitor in vitro and in vivo.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3