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Purity: ≥98%
Dapsone (Diaphenylsulfone; Sulfona) is a synthetic derivative of diamino-sulfone which is active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae. Dapsone has anti-inflammatory and anti-bacterial properties, commonly used for the treatment of leprosy. It is a second-line medication for the treatment and prevention of Pneumocystis pneumonia and for the prevention of toxoplasmosis in those who have poor immune function. Additionally, it has been used for acne as well as other skin conditions. Dapsone is available both topically and by mouth. As a structural analog of p-aminobenzoic acid (PABA), dapsone inhibits dihydropteroate synthase (DHPS), an enzyme important in folate synthesis, resulting in a depletion of the folate pool and a reduction in the amount of thymidylate available for DNA synthesis.
Targets |
bacteriostatic; folate synthesis
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ln Vitro |
Once 100 μg of protein has been added to cell lysates, dapsone is tested using the DHPS activity assay. In the DHPS activity assay, Dapsone has an IC50 of 3.0 μg/ml for E. Coli C600; however, at 256 μg/ml, Dapsone does not inhibit the growth of E. Coli C600. IC50 and MIC values for Dapsone for the recombinant strain containing M. leprae folP1 (pML101) are 0.06 μg/ml and 1 μg/ml, respectively[2].
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ln Vivo |
Dapsone (topical treatment; 50 mg/kg; twice daily; 30 days) causes lesions to be about 186 mm2 in size in BALB/c mice infected with L. major as opposed to 125 mm2 in control mice. Moreover, 9.6±8.5 µg of DAP/mg of skin was measured for the lesions treated with DAP cream. But compared to mice that were not given the cream, the amount of parasites discovered in the spleen was noticeably reduced in the mice that received the cream[3].
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References |
Molecular Formula |
C12H12N2O2S
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Molecular Weight |
248.3009
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Exact Mass |
248.06
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Elemental Analysis |
C, 58.05; H, 4.87; N, 11.28; O, 12.89; S, 12.91
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CAS # |
80-08-0
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Related CAS # |
Dapsone-d8;557794-38-4;Dapsone-d4;1346602-12-7;Dapsone-13C12;1632119-29-9
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Appearance |
Solid powder
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SMILES |
C1=CC(=CC=C1N)S(=O)(=O)C2=CC=C(C=C2)N
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InChi Key |
MQJKPEGWNLWLTK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C12H12N2O2S/c13-9-1-5-11(6-2-9)17(15,16)12-7-3-10(14)4-8-12/h1-8H,13-14H2
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Chemical Name |
4-(4-aminophenyl)sulfonylaniline
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Synonyms |
Diaphenylsulfone; 4,4'-Sulfonyldianiline; 4,4'-Diaminodiphenyl sulfone; Sulfona; 4,4′-Diaminodiphenyl sulfone; DDS
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 49~250 mg/mL ( 197.34~1006.85 mM )
Ethanol : ~10 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (10.07 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0274 mL | 20.1369 mL | 40.2739 mL | |
5 mM | 0.8055 mL | 4.0274 mL | 8.0548 mL | |
10 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.