Name: Sulfaphenazole
Price: 286.00 USD

- Overview
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    Background
    
    Sulfaphenazole is a strong and competitive inhibitor of CYP2C9 [1]. CYP2C9 is a major cytochrome P450 enzyme involved in the metabolic clearance of various therapeutic agents, such as oral anticoagulants, nonsteroidal anti-inflammatories, and oral hypoglycemics. Disruption of CYP2C9 activity results in many adverse drug reactions [2].In vitro: In yeast expressed human cytochromes P450 of the 1A, 3A, and 2C subfamilies, sulfaphenazole acts as a strong and competitive inhibitor of CYP 2C9 with the Ki value of 0.3 ± 0.1 μM. The Ki values of sulfaphenazole for CYP 2C8 and 2C18 were 63 and 29 μM, respectively. Sulfaphenazole failed to inhibit CYP 1A1, 1A2, 3A4, and 2C19 [1]. In vivo: In diabetic male mice (db/db strain), daily intraperitoneal injections of either the CYP 2C inhibitor sulfaphenazole (5.13 mg/kg) for 8 weeks, sulfaphenazole restored endothelium-mediated relaxation in db/db mice. Sulfaphenazole reduced oxidative stress, increased NO bioavailability and restored endothelial function in db/db mice [3].
    
    [1] Mancy A, Dijols S, Poli S, et al. Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: molecular origin of the specific inhibitory effects of sulfaphenazole on CYP 2C9 and consequences for the substrate binding site topology of CYP 2C9[J]. Biochemistry, 1996, 35(50): 16205-16212.
    [2] Rettie A E, Jones J P. Clinical and toxicological relevance of CYP2C9: drug-drug interactions and pharmacogenetics[J]. Annu. Rev. Pharmacol. Toxicol., 2005, 45: 477-494.
    [3] Elmi S, Sallam N A, Rahman M M, et al. Sulfaphenazole treatment restores endothelium-dependent vasodilation in diabetic mice[J]. Vascular pharmacology, 2008, 48(1): 1-8.
- Properties
  - Alternative Name
    
    Depocid,Depotsulfonamide,Plisulfan,Raziosulfa; 4-amino-N-(1-phenyl-1H-pyrazol-5-yl)-benzenesulfonamide
    
    CAS Number
    
    526-08-9
    
    Molecular Formula
    
    C15H14N4O2S
    
    Molecular Weight
    
    314.4
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥13.15 mg/mL in DMSO; ≥9.92 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Sulfaphenazole

Sulfaphenazole

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