| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
|
||
| Other Sizes |
| ln Vitro |
In rheumatoid arthritis (RA) synoviocytes, sulfapyridine suppresses the synthesis of IL-8, chemokine (CXC motif) ligand 1 (CXCL1), and monocyte chemoattractant protein 1 (MCP-1)[1]. Sulfapyridine has a minimum inhibitory concentration (MIC) range of 3.1–25 μg/mL for Yersinia enterocolitica and 25–100 μg/mL for Salmonella. Salmonella jejuni/E. Sulfapyridine has a lower susceptibility to coli, with MIC values ranging from 200 to 800 μg/mL. Three of the five E. Coli and Shigella. Sulfapyridine at 1600 μg/mL did not affect the coli strains. For two E, 25 μg/mL inhibits. strains of Coli [2].
|
|---|---|
| ln Vivo |
In rats, compound 48/80 elicited a systemic allergic reaction that was greatly reduced by sulfapyridine (1 and 10 μg/kg; intraperitoneal injection) [4].
|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Approximately 60-80% of the metabolism/metabolites are metabolized by the liver. Known metabolites of sulfapyridine include sulfapyridine N-acetyl. Biological Half-Life: 6-14 hours. |
| Toxicity/Toxicokinetics |
Protein Binding
Approximately 50% is bound to plasma proteins. |
| References |
|
| Additional Infomation |
Sulfapyridine is an odorless or nearly odorless white or pale yellow crystalline powder with a slightly bitter taste. Its aqueous solution is neutral. (NTP, 1992)
Sulfapyridine is a sulfonamide compound consisting of a pyridine ring with a 4-aminobenzenesulfonamide group attached at the 2-position. It is used as an anti-infective agent, dermatological drug, xenobiotic, environmental pollutant, and drug allergen. It belongs to the pyridine, sulfonamide, substituted aniline, and sulfonamide antibiotic classes. Its function is related to sulfonamide compounds. It has antibacterial activity but may be toxic; it was once used to treat certain skin diseases. It is now discontinued. Sulfapyridine is a short-acting sulfonamide antibiotic, a byproduct of the nonsteroidal anti-inflammatory drug sulfasalazine. Its production and use were discontinued in 1990. An antibacterial drug, possibly toxic, used to treat certain skin diseases. See also: Sulfapyridine sodium (in salt form). Indications For the treatment of dermatitis herpetiformis, benign mucosal pemphigoid, and pyoderma gangrenosa. Mechanism of Action Sulfapyridine is a competitive inhibitor of bacterial dihydropteranoic acid synthase. Inhibition of this enzyme is crucial for these organisms to synthesize folic acid by processing the substrate para-aminobenzoic acid (PABA). The activity of dihydropteranoic acid synthase is essential for folic acid synthesis, which is necessary for the synthesis of nucleic acids such as DNA or RNA by cells. Therefore, if DNA molecules cannot be synthesized, cells cannot divide. Pharmacodynamics Sulfapyridine is a sulfonamide antibiotic. Sulfonamides are synthetic antibacterial antibiotics with broad-spectrum antibacterial activity against most Gram-positive bacteria and many Gram-negative bacteria. However, many strains of the same bacterial species may develop resistance. Sulfonamides inhibit bacterial growth by competitively inhibiting para-aminobenzoic acid in the folic acid metabolic cycle. Bacteria exhibit similar sensitivity to various sulfonamides; resistance to one sulfonamide implies resistance to all sulfonamides. Most sulfonamides are well absorbed orally. However, parenteral administration is challenging due to the strong alkalinity and tissue irritation of soluble sulfonamide salts. Sulfonamides are widely distributed in all tissues. High concentrations can be reached in pleural fluid, peritoneal fluid, synovial fluid, and ocular fluid. Although these drugs are no longer used to treat meningitis, high concentrations remain in the cerebrospinal fluid of patients with meningeal infections. Pus can inhibit their antibacterial activity. |
| Molecular Formula |
C11H11N3O2S
|
|---|---|
| Molecular Weight |
249.288
|
| Exact Mass |
249.057
|
| CAS # |
144-83-2
|
| Related CAS # |
Sulfapyridine-d4;1189863-86-2
|
| PubChem CID |
5336
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
473.5±51.0 °C at 760 mmHg
|
| Melting Point |
191-193°C
|
| Flash Point |
240.2±30.4 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.674
|
| LogP |
0.03
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
17
|
| Complexity |
331
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GECHUMIMRBOMGK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H11N3O2S/c12-9-4-6-10(7-5-9)17(15,16)14-11-3-1-2-8-13-11/h1-8H,12H2,(H,13,14)
|
| Chemical Name |
4-amino-N-pyridin-2-ylbenzenesulfonamide
|
| Synonyms |
A-499; A499; A 499
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~60 mg/mL (~240.68 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (12.03 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 30.0 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: ≥ 3 mg/mL (12.03 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 30.0 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: ≥ 3 mg/mL (12.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0114 mL | 20.0570 mL | 40.1139 mL | |
| 5 mM | 0.8023 mL | 4.0114 mL | 8.0228 mL | |
| 10 mM | 0.4011 mL | 2.0057 mL | 4.0114 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.