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Purity: ≥98%
Olsalazine Sodium (CJ-91B) is a potent anti-inflammatory prodrug, which consists of two 5-ASA moieties linked by an azo bond.Olsalazine displays multiple effects on intestinal electrolyte. The ileal mucosa of rats and rabbits exhibits increased secretion of both sodium and chloride ions and decreased absorption of chloride ions when Olsalazine (< 2.89 mM) is applied in vitro. In addition, dose-dependent reductions in net sodium and, to a greater extent, chloride absorption are observed in the isolated rat colon at concentrations of Olsalazine < 11.5 mM. Only at a high Olsalazine concentration (11.5 mM) does potassium secretion increase as well.
| ln Vitro |
Olsalazine affects intestinal electrolyte in a number of ways. When Olsalazine (< 2.89 mM) is applied in vitro, the ileal mucosa of rats and rabbits secretes more sodium and chloride ions and absorbs less of them. In the isolated rat colon, concentrations of olsalazine less than 11.5 mM also reduce net sodium and, to a greater extent, chloride absorption in a dose-dependent manner. The secretion of potassium also increases, but only up to a high concentration of 11.5 mM Olsalazine. In isolated rat jejunum, olsalazine also prevents the absorption of lactose and glucose.[1] Olsalazine, having an IC50 of 0.39 mM, is a strong inhibitor of the chemotaxis of human intestinal macrophages to LTB4. **[2]** By reduction of 31% and 73%, respectively, olsalazine (0.4 mM) inhibits the production of superoxide radicals produced by xanthine-xanthine oxidase reaction or by neutrophils activated by phorbol myristate acetate (PMA).[3] Further proposed mechanisms through which mesalazine derived from olsalazine may alleviate mucosal mucosa/inflammatory colonic conditions include suppression of colonic fatty acid oxidation, inhibition of platelet activating factor, inhibition of cytokine production in human mononuclear cells, inhibition of endothelial cell proliferation by folic acid antagonism, inhibition of leukotriene synthesis from arachidonic acid via inhibition of lipoxygenase, as well as other potential mechanisms.[4] modification of the prostaglandin profile through interference with leukocyte function and prostaglandin 15-hydroxydehydrogenase [5]. [6]
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| ln Vivo |
Olsalazine was created as a means of getting mesalazine into the colon because, when taken orally, very little of the parent molecule is absorbed from the gastrointestinal tract. Azole bonds are broken down in the colon by azoreductase bacteria, releasing two molecules of mesalazine that have been shown to be therapeutically effective in treating inflammatory bowel disorders. [1] Experimental colitis induced by dextran sulphate sodium in nu/nu CD-1 mice is significantly prolonged in survival when ossalazine (50 mg/kg/day) is administered. [7] Tumor growth is inhibited by olsalazine in a rodent model of colorectal cancer. Olsalazine (25 mg/kg/day) reduces the number and volume of tumors in rats treated with 1,2-dimethylhydrazine by 58.17% and 62.67%, respectively. When olsalazine is administered, the number of apoptotic cells increases 1.7 times, and the rate of cell proliferation decreases by 42.4%. [8]
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| Animal Protocol |
Primary colonic tumors induced with DMH
25 mg/kg/day Administered in food |
| References |
[1]. Drugs . 1991 Apr;41(4):647-64. [2]. Aliment Pharmacol Ther . 1988 Jun;2(3):203-11. [3]. Dig Dis Sci . 1991 Feb;36(2):174-8. [4]. Dig Dis Sci . 1987 Jun;32(6):577-82. [5]. Dig Dis Sci . 1985 Dec;30(12):1161-5. [6]. Acta Med Scand . 1979;206(6):451-7. |
| Molecular Formula |
C14H8N2NA2O6
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| Molecular Weight |
346.2
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| Exact Mass |
302.05
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| Elemental Analysis |
C, 48.57; H, 2.33; N, 8.09; Na, 13.28; O, 27.73
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| CAS # |
6054-98-4
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| Related CAS # |
Olsalazine; 15722-48-2
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=C(C=C1N=NC2=CC(=C(C=C2)[O-])C(=O)O)C(=O)O)[O-].[Na+].[Na+]
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| InChi Key |
ZJEFYLVGGFISGT-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C14H10N2O6.2Na/c17-11-3-1-7(5-9(11)13(19)20)15-16-8-2-4-12(18)10(6-8)14(21)22;;/h1-6,17-18H,(H,19,20)(H,21,22);;/q;2*+1/p-2
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| Chemical Name |
disodium;2-carboxy-4-[(3-carboxy-4-oxidophenyl)diazenyl]phenolate
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 15 mg/mL (43.33 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8885 mL | 14.4425 mL | 28.8850 mL | |
| 5 mM | 0.5777 mL | 2.8885 mL | 5.7770 mL | |
| 10 mM | 0.2889 mL | 1.4443 mL | 2.8885 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00004288 | Completed | Drug: olsalazine | Ankylosing Spondylitis | National Center for Research Resources (NCRR) |
May 1996 | Phase 2 |
Products are for research use only; We do not sell to patients
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