Sulfaphenazole (Synonyms: Depocid,Depotsulfonamide,Plisulfan,Raziosulfa) |
| رقم الكتالوجGC11638 |
السلفافينازول هو مثبط محدد لـ CYP2C9 الذي يمنع التأثيرات المسببة للالتهاب وتصلب الشرايين لحمض اللينوليك (زيادة الإجهاد التأكسدي وتنشيط AP-1) بوساطة CYP2C9
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 526-08-9
Sample solution is provided at 25 µL, 10mM.
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Sulfaphenazole is a sulfonamide antibacterial drug. It competitively inhibits bacterial dihydrofolate synthase, blocking bacterial folate synthesis and thereby inhibiting bacterial growth and reproduction [1]. Sulfaphenazole is a selective inhibitor of the human cytochrome P450 (CYP) 2C9 enzyme [2]. Sulfaphenazole is a cytoprotective agent that prevents light-induced photoreceptor cell death. Sulfaphenazole inhibits light-induced necrosis and apoptosis triggered by mitochondrial stress [3].
In yeast expressed human cytochromes P450 of the 1A, 3A, and 2C subfamilies, Sulfadilamide acts as a strong and competitive inhibitor of CYP 2C9 with the Ki value of 0.3±0.1μM. The Ki values of Sulfadilamide for CYP 2C8 and 2C18 were 63 and 29μM, respectively. Sulfaphenazole failed to inhibit CYP 1A1, 1A2, 3A4, and 2C19 [2]. Sulfaphenazole (10μM; 1h) causes the numbers of light-induced apoptotic and necrotic cells decreased by 33 and 44%, respectively[3].
In a model of Diabetic male mice (db/db strain), Sulfaphenazole(5.13mg/kg; po; 8 weeks) reduces oxidative stress (measured as plasma levels of 8-isoprostane), increases NO bioavailability (measured as NO2−), and restores endothelial function in db/db mice without affecting plasma glucose levels [4]. Sulfaphenazole (100µL; ip; 15d) exposure post-injury was found to improve tissue perfusion in mouse models of both thermal injury and I/R-induced pressure injury, leading to reduced overall severity, improved wound closure and increased scar tensile strength [5]. In a rat model of myocardial ischemia-reperfusion (I/R) injury, Sulfaphenazole (30mg/kg; iv) treatment restored cardiac function and reduced myocardial infarct size. Furthermore, Sulfaphenazole reduced superoxide anion levels and enhanced NO bioavailability in reperfused hearts [6]. In a rat model of acute myocardial infarction (MI), Sulfaphenazole (8.1mg/kg; ip; 3d) pretreatment of rats with ameliorated I=R-induced myocardial damage and improved cardiac contractile functions by decreasing superoxide production, peroxynitrite formation, and by enhancing NO bioavailability, myocardial tissue oxygenation, and iNOS expression [7].
References:
[1].Elmongy E I, Alanazi W S, Aldawsari A I, et al. Antimicrobial evaluation of sulfonamides after coupling with thienopyrimidine coplanar structure[J]. Pharmaceuticals, 2024, 17(2): 188.
[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(1): 477-494.
[3]. Bogaard J, Chang Q, Berdyshev E A, et al. Cytochrome P450 2C Inhibitors Protect Photoreceptors from Light Induced Cell Death[J]. Investigative Ophthalmology & Visual Science, 2014, 55(13): 4387-4387.
| Cell experiment [1]: | |
Cell lines | 661W cells |
Preparation Method | 661W cells were seeded onto 96 well plates and given 9-cis retinal overnight to sensitize them to light. Cells were then given serum free media with/without a compound of interest. The 661W cells were pretreated with 10μM Sulfaphenazole for 1 hour.Then cells were exposed to 11,000 lux of light to inflict cell death. Media fractions and lipid extracts were obtained following light exposure to perform lipid profiling using LC/MS. |
Reaction Conditions | 10 μM; 1h |
Applications | Sulfaphenazole (10 μM; 1h) causes the numbers of light-induced apoptotic and necrotic cells decreased by 33 and 44%, respectively. |
| Animal experiment [2]: | |
Animal models | Diabetic male mice (db/db strain) |
Preparation Method | Diabetic male mice (db/db strain) and their age-matched controls received daily intraperitoneal injections of either the CYP 2C inhibitor sulfaphenazole (5.13mg/kg) or saline (vehicle control) for 8 weeks. |
Dosage form | 5.13mg/kg; po; 8 weeks |
Applications | Sulfaphenazole reduces oxidative stress (measured as plasma levels of 8-isoprostane), increases NO bioavailability (measured as NO2−), and restores endothelial function in db/db mice without affecting plasma glucose levels. |
References: | |
| Cas No. | 526-08-9 | SDF | |
| المرادفات | Depocid,Depotsulfonamide,Plisulfan,Raziosulfa | ||
| Chemical Name | 4-amino-N-(1-phenyl-1H-pyrazol-5-yl)-benzenesulfonamide | ||
| Canonical SMILES | NC1=CC=C(S(NC2=CC=NN2C3=CC=CC=C3)(=O)=O)C=C1 | ||
| Formula | C15H14N4O2S | M.Wt | 314.4 |
| الذوبان | ≥ 13.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1807 mL | 15.9033 mL | 31.8066 mL |
| 5 mM | 636.1 μL | 3.1807 mL | 6.3613 mL |
| 10 mM | 318.1 μL | 1.5903 mL | 3.1807 mL |
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Quality Control & SDS
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- Purity: >98.50%
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