| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 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
◉ Summary of Use during Lactation Although no information exists on the excretion of balsalazide into breastmilk, it is metabolized to the active drug mesalamine. A few cases of diarrhea have been reported in infants exposed to mesalamine, although the rate is not high. Most experts and professional guidelines consider mesalamine derivatives to be acceptable during breastfeeding. If balsalazide is required by the mother, it is not a reason to discontinue breastfeeding, but observe breastfed infants for diarrhea. ◉ Effects in Breastfed Infants The active metabolite of balsalazide, mesalamine, was probably responsible for diarrhea in a 6-week-old whose diarrhea recurred 4 times after rechallenging of the mother 4 times during breastfeeding. In a prospective telephone follow-up study, 8 nursing mothers reported taking mesalamine (dosage and route unspecified). One mother reported diarrhea in her infant. No other adverse reactions were reported in the infants by their mothers. A case-control study compared the infants of mothers taking mesalamine (n = 117; average dose, 2065 mg daily), olsalazine (n = 2) or sulfasalazine (n = 2) to infants of matched control mothers (n = 121) who were exposed to no treatment known to be harmful to a breastfed infant. Infants were exposed to mesalamine through milk for a mean of 5.3 months (range: 3 days-24 months). Infants were breastfed for an average of about 7.4 months and were followed up at an average age of about 22 months. No difference in the frequency or characteristics of maternally reported adverse events were found between exposed and control infants. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Balsalazide is a monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond. It has a role as a prodrug, a non-steroidal anti-inflammatory drug, an anti-ulcer drug and a gastrointestinal drug. It is a conjugate acid of a balsalazide(2-).
Balsalazide is an Aminosalicylate. See also: Balsalazide (annotation moved to); Balsalazide Disodium (annotation moved to). |
| 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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