| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Salazopyridazine is an anti-inflammatory agent with multiple mechanisms. It is a prodrug that is cleaved by gut bacteria into 5-ASA and a pyridazine-containing sulfonamide. 5-ASA is a topical anti-inflammatory agent in the colon, acting as an antioxidant and inhibitor of NF-kappaB and other inflammatory pathways. The sulfonamide moiety also contributes to immunosuppressive effects.
|
|---|---|
| ln Vitro |
In vitro, Salazopyridazine has been shown to possess antibacterial properties and inhibitory effects in models of ulcerative colitis. The exact IC₅0 values for specific targets are not detailed here. Its primary activity is believed to be the anti-inflammatory effect of its 5-ASA metabolite, which reduces the production of inflammatory mediators like prostaglandins and leukotrienes in the colonic mucosa.
|
| ln Vivo |
In vivo, Salazopyridazine has demonstrated inhibitory effects on ulcerative colitis in animal models. It has been studied for its potential to treat rheumatic diseases. As a prodrug, it is designed to be poorly absorbed in the upper gastrointestinal tract, allowing it to reach the colon where it is activated, thus concentrating the therapeutic effect in the large intestine for bowel diseases.
|
| Enzyme Assay |
A non-cellular assay to study its mechanism would be to measure the inhibition of NF-kappaB activation. A standard approach is an electrophoretic mobility shift assay (EMSA). The active metabolite 5-ASA is incubated with isolated nuclear extracts from stimulated cells. The ability of the compound to prevent the binding of the NF-kappaB transcription factor to a radiolabeled DNA oligonucleotide probe can be assessed. This provides a direct measure of its inhibition of inflammatory gene transcription.
|
| Cell Assay |
A cellular assay to assess its in vitro anti-inflammatory effect uses intestinal epithelial cells or immune cells. Cells (e.g., human colon carcinoma cell line Caco-2) are stimulated with an inflammatory cytokine such as TNF-alpha to induce expression of inflammatory genes (e.g., IL-8). The cells are pre-treated with Salazopyridazine or its 5-ASA metabolite. After a period of incubation, the concentration of IL-8 in the cell culture supernatant is measured using an ELISA kit to quantify the anti-inflammatory effect.
|
| Animal Protocol |
In vivo animal studies for colitis are typically performed in a rodent model of inflammatory bowel disease (IBD). A common method is the dextran sulfate sodium (DSS)-induced colitis model. Mice are given DSS in their drinking water for 5-7 days to induce severe colitis. During this period, Salazopyridazine is administered either orally or rectally. The therapeutic effect is assessed by daily measurement of body weight, stool consistency, and fecal occult blood, culminating in a "disease activity index" (DAI) score. After euthanasia, the colon length is measured (a marker of inflammation) and tissue is taken for histopathological scoring.
|
| ADME/Pharmacokinetics |
The pharmacokinetics of Salazopyridazine follow the typical pattern of a sulfasalazine-like drug. Its oral bioavailability is low, as it is designed to be minimally absorbed. The majority of an oral dose reaches the colon, where it is cleaved by bacterial azoreductases. The 5-ASA metabolite acts topically and is minimally absorbed. The pyridazine-sulfonamide moiety may be absorbed. The drug is used in chronic inflammatory conditions.
|
| Toxicity/Toxicokinetics |
The safety profile of Salazopyridazine is likely similar to other sulfa drugs. Common adverse effects include gastrointestinal disturbances (nausea, loss of appetite), headache, and rash. More serious but rare effects include hepatotoxicity, blood dyscrasias (e.g., agranulocytosis), and Stevens-Johnson syndrome. It is not recommended for patients with sulfonamide allergy.
|
| References |
[1]. Sigidin IaA. Institut Revmatizma RAMN i progress antirevmaticheskoĭ terapii [Institute of Rheumatology and progress of antirheumatic therapy]. Vestn Ross Akad Med Nauk. 1998;(12):7-9.
[2]. Belohlavek D, et al. Entzündliche Darmerkrankungen Colitis ulcerose und M. Crohn. Frühdiagnose und Behandlung [Inflammatory intestinal diseases: ulcerative colitis and Crohn's disease. Early diagnosis and treatment]. Fortschr Med. 1976 Mar 4;94(7):358-62. |
| Additional Infomation |
Salazopyridazine has a unique mechanism that relies on the colonic microbiome for activation. This drug is an azo compound. It is not a currently approved first-line therapy and is considered an older or research compound. Its use has been largely superseded by newer, more specific biologics for the treatment of IBD, but it remains a valuable research tool and has been used in clinical studies, particularly in Eastern Europe.
|
| Molecular Formula |
C18H15N5O6S
|
|---|---|
| Molecular Weight |
429.41
|
| Exact Mass |
429.074
|
| CAS # |
22933-72-8
|
| PubChem CID |
65707
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.54g/cm3
|
| Boiling Point |
703.9ºC at 760mmHg
|
| Flash Point |
379.5ºC
|
| Vapour Pressure |
8.54E-21mmHg at 25°C
|
| Index of Refraction |
1.693
|
| LogP |
4.259
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
30
|
| Complexity |
706
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=NN=C(C=C1)NS(=O)(=O)C2=CC=C(C=C2)N=NC3=CC(=C(C=C3)O)C(=O)O
|
| InChi Key |
YFUATOCFMCWUEH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H15N5O6S/c1-29-17-9-8-16(21-22-17)23-30(27,28)13-5-2-11(3-6-13)19-20-12-4-7-15(24)14(10-12)18(25)26/h2-10,24H,1H3,(H,21,23)(H,25,26)
|
| Chemical Name |
2-hydroxy-5-[[4-[(6-methoxypyridazin-3-yl)sulfamoyl]phenyl]diazenyl]benzoic acid
|
| 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 : 125 mg/mL (291.10 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3288 mL | 11.6439 mL | 23.2878 mL | |
| 5 mM | 0.4658 mL | 2.3288 mL | 4.6576 mL | |
| 10 mM | 0.2329 mL | 1.1644 mL | 2.3288 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
