| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| ln Vivo |
Balsalazide is a new 5-aminosalicylic acid (5-ASA) prodrug [2]. At endpoint, protein production of MIP-1β, MCP-1, IL-6, and IL-10 in colon tissue decreased with plasma concentrations of the cytokines. Additionally, the drug treatment group showed lower expression of p-STAT3 compared with the CAC group, and BCL2 was significantly reduced and BAX was significantly increased.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation While there is currently no information on whether balsalazine is excreted into breast milk, it is metabolized in breast milk to the active drug mesalazine. A small number of infants have been reported to experience diarrhea after taking mesalazine, but the incidence is low. Most experts and professional guidelines consider mesalazine derivatives safe for breastfeeding women. ◉ Effects on Breastfed Infants Mesalazine, the active metabolite of balsalazine, may have been the cause of diarrhea in a 6-week-old infant who experienced four recurrences of diarrhea after the mother took balsalazine four times during breastfeeding. In a prospective telephone follow-up study, eight breastfeeding mothers reported taking mesalazine (dosage and route of administration not specified). One mother reported diarrhea in her infant. No other adverse reactions were reported in the infants by the mothers. A case-control study compared infants born to mothers receiving mesalazine (n = 117; mean dose, 2065 mg daily), olsalazine (n = 2), or sulfasalazine (n = 2) with infants born to a mother-matched control group (n = 121). Control group mothers did not receive any treatment known to be harmful to breastfed infants. The mean duration of breastfeeding exposure to mesalazine was 5.3 months (range: 3 days to 24 months). Infants were breastfed for approximately 7.4 months on average and followed up at a mean of approximately 22 months of age. There were no differences in the frequency or characteristics of maternally reported adverse events between the exposed and control groups. ◉ Effects on breastfeeding and breast milk As of the revision date, no relevant published information was found. |
| References |
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| Additional Infomation |
Balsalazine is a monohydroxybenzoic acid composed of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-β-alanine via an azo bond. It is used as a prodrug, nonsteroidal anti-inflammatory drug, anti-ulcer agent, and gastrointestinal medication. It is the conjugate acid of balsalazine (2-). Balsalazine is an aminosalicylic acid salt. See also: Balsalazine (note moved to); Balsalazine disodium (note moved to).
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| Exact Mass |
357.096
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|---|---|
| CAS # |
80573-04-2
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| Related CAS # |
Balsalazide sodium hydrate;150399-21-6;Balsalazide-d4;2714315-25-8
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| PubChem CID |
54585
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| Appearance |
Yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
254-255ºC
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| Index of Refraction |
1.650
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| LogP |
1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
545
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C(O)=CC=C(/N=N/C2C=CC(C(=O)NCCC(=O)O)=CC=2)C=1)(=O)O
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| InChi Key |
IPOKCKJONYRRHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15N3O6/c21-14-6-5-12(9-13(14)17(25)26)20-19-11-3-1-10(2-4-11)16(24)18-8-7-15(22)23/h1-6,9,21H,7-8H2,(H,18,24)(H,22,23)(H,25,26)
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| Chemical Name |
5-[[4-(2-carboxyethylcarbamoyl)phenyl]diazenyl]-2-hydroxybenzoic acid
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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 : ~100 mg/mL (~279.86 mM)
1M NaOH : 50 mg/mL (~139.93 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.00 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 (7.00 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. (Please use freshly prepared in vivo formulations for optimal results.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00618202 | COMPLETED | Drug: Balsalazide | Ulcerative Colitis | Roxane Laboratories | 2005-05 | Not Applicable |
| NCT00618228 | COMPLETED | Drug: Balsalazide | Ulcerative Colitis | Roxane Laboratories | 2004-01 | Not Applicable |
| NCT00486031 | COMPLETEDWITH RESULTS | Drug: Balsalazide Disodium | Inflammatory Bowel Disease Ulcerative Colitis |
Bausch Health Americas, Inc | 2006-10 | Phase 3 |
| NCT00408174 | COMPLETED | Drug: Balsalazide disodium | Inflammatory Bowel Disease Ulcerative Colitis |
Bausch Health Americas, Inc | 2006-05 | Phase 3 |
| NCT00649480 | COMPLETED | Drug: BALSALAZIDE DISODIUM CAPSULES, 750 MG Drug: COLAZAL® Capsules 750 mg |
Healthy | Mylan Pharmaceuticals Inc | 2007-01 | Phase 1 |
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