Sulfaphenazole
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Storage | Store at -20°C |
M.Wt | 314.4 |
Cas No. | 526-08-9 |
Formula | C15H14N4O2S |
Synonyms | Depocid,Depotsulfonamide,Plisulfan,Raziosulfa |
Solubility | insoluble in H2O; ≥13.15 mg/mL in DMSO; ≥9.92 mg/mL in EtOH with ultrasonic |
Chemical Name | 4-amino-N-(1-phenyl-1H-pyrazol-5-yl)-benzenesulfonamide |
SDF | Download SDF |
Canonical SMILES | NC1=CC=C(S(NC2=CC=NN2C3=CC=CC=C3)(=O)=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |