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Sulfanilamide Europäischer Partner

Hersteller Selleckchem
Kategorie
Typ Inhibitors
Specific against other
Menge 50 mg
ArtNr S1685-50
CAS-Nr. 63-74-1
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Administration
Orally taken every day
Animal Models
Male Sprague-Dawley rats
Description
Sulfanilamide (Sulphanilamide) is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 uM.
Dosages
100 mg/kg
Formulation
Thoroughly mixed into the daily ration of pulverized food and compounded into pellets.
IC50
320 uM [1], 320 uM [1], 320 uM [1], 320 uM [1], 320 uM [1], 320 uM [1]
In vitro
Sulfanilamide containing the sulfonamide functional group displays inhibitory activity for dihydropteroate synthetase partially purified from Escherichia coli which normally uses para-aminobenzoic acid (PABA) for synthesizing the necessary folic acid acting as a coenzyme in the synthesis of purine, pyrimidine and other amino acids, exhibiting an IC 50 of 320 uM for dihydropteroate synthetasea and Km of 2.5 uM for PABA. [1] Sulfanilamide shows IC50 of 286.8 ug/mL for recombinant S. cerevisiae strains with wild-type FOL1 genes, but the single mutation 55Trp to 55Ala or 57Pro to 57Ser within the putative active site of the fungal DHPS confers resistance to Sulfanilamide with IC50 of >800 ug/mL. [2] Sulfanilamide moderately inhibits the growth of bacterial cells harboring plasmodium falciparum pKOS-pfPPPK-DHPS (His) with IC50 of 380 uM. [3]
In vivo
Administration of Sulfanilamide with the dosage of 100 mg/kg/day is effective in the prevention of P. carinii infection in the immunosuppressed rat model. When the dosage of sulfaguanidine and Sulfanilamide reduced to 10 mg/kg/day, breakthrough P. carinii infection occurs in the rats. [4]
Kinase Assay
Assay of dihydropteroate synthetase activity, The dihydropteroate synthetase activity is measured by a modification of the radioactive assay based on the incorporation of 14C-PABA into dihydropteroate. The reaction mixture in test tubes (1 by 7 cm) is prepared in 0.4 mL of 100 mM Tris-HCl buffer (pH 8.5) (containing 10 mM of MgCl2, 50 mM of 2-ME, 0.12 mM of hydroxymethyldihydropteridine pyrophosphate, 0.01 mM of 14C-PABA, a set of concentrations of Sulfanilamide and 0.2 mg partially purified dihydropteroate synthetase extract), and incubated for 1 hour at 37 C. The reactions are stopped immediately by the addition of 25 uM of EDTA (pH 8.3) to each reaction mixture, then evaporated to dryness under reduced pressure and redissolved in 0.075 mL of 0.05 M Tris (pH 8.0). 0.05 mL of the above mixture is applied (each in an area of 1.0 by 4.0 cm) to Whatman 3MM chromatography paper. The chromatograms are developed by descending chromatography with 0.1 M potassium phosphate buffer (pH 7.0), for 4 hours at 25 C. Under these conditions, pteroate (dihydropteroate is oxidized to pteroate during the evaporation step) remains at the origin, whereas unreacted 14C-PABA migrates with an Rf value of 0.78. Areas corresponding to the origin of the developed chromatograms are cut out and counted in a liquid scintillation counter. The concentration of Sulfanilamide required for 50% inhibition of dihydropteroate synthetase activity represents IC50.
Molecular Weight (MW)
172, 2
Picture ChemicalStructure Description
Sulfanilamide Chemical Structure
Solubility (25C)
DMSO 34 mg/mL, Water <1 mg/mL, Ethanol 17 mg/mL
Storage
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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Menge: 50 mg
Lieferbar: In stock
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Lieferung vsl. bis 11.04.2024 

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