Sulfaphenazole

SKU: orb1222105

Description

Sulfaphenazole is an inhibitor of CYP2C9 (Ki: 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 μM for CYP2C8/CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). At 10 μM, sulfaphenazole has been shown to inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 526-08-9
• MW: 314.36
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₄N₄O₂S
• SMILES: Nc1ccc(cc1)S(=O)(=O)Nc1ccnn1-c1ccccc1
• Target: GSK-3
• Solubility: DMSO : ≥ 100 mg/mL; 318.11 mM

Bioactivity

• In Vivo:
  Animal model: Diabetic male mice (db/db strain). Dosage: 5.13 mg/kg. Administration: Intraperitoneal injections; daily; for 8 weeks. Result: Although sulfaphenazole did not change endothelium-dependent vasodilation in control mice, it restored endothelium-mediated relaxation in db/db mice.
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• In Vitro:
  Apoptosis Analysis Cell line: 661W cells. Concentration: 10 μM. Incubation time: For 1 h at 37 °C followed by light exposure for 2-3 h. Result: The numbers of light-induced apoptotic and necrotic cells were decreased by 33 and 44%, respectively.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRN-0308518 | Sulfaphenazole | Firmazolo | Inamil

Quick Database Links

Gene Symbol

GSK-3