Sulfaphenazole (Synonyms: Depocid,Depotsulfonamide,Plisulfan,Raziosulfa) |
| Catalog No.GC11638 |
CYP2C9 inhibitor
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 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].
References:
[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.
| Cas No. | 526-08-9 | SDF | |
| Synonyms | 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 |
| Solubility | ≥ 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. |
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| 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 | 0.6361 mL | 3.1807 mL | 6.3613 mL |
| 10 mM | 0.3181 mL | 1.5903 mL | 3.1807 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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