Olsalazine sodium | CAS#6054-98-4| Anti-inflammatory drug

MedKoo Cat#: 318386 | Name: Olsalazine sodium

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Olsalazine is an anti-inflammatory drug used in the treatment of inflammatory bowel disease such as ulcerative colitis. Like balsalazide, olsalazine is believed to deliver mesalazine, or 5-aminosalicylic acid (5-ASA), past the small intestine, directly to the large intestine, which is the active site of disease in ulcerative colitis.

Chemical Structure

Olsalazine sodium

CAS#6054-98-4 (sodium)

Theoretical Analysis

MedKoo Cat#: 318386

Name: Olsalazine sodium

CAS#: 6054-98-4 (sodium)

Chemical Formula: C14H8N2Na2O6

Exact Mass: 302.0539

Molecular Weight: 346.02

Elemental Analysis: C, 48.57; H, 2.33; N, 8.09; Na, 13.28; O, 27.73

Price and Availability

Size	Price	Availability
200mg	USD 230.00	2 Weeks
500mg	USD 350.00
1g	USD 550.00
2g	USD 950.00	2 Weeks
5g	USD 1,650.00	2 Weeks

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Related CAS #

15722-48-2 (free acid) 6054-98-4 (sodium)

Synonym

Olsalazine, Dipentum, Azodisal sodium, Azodisalicylate, CJ-91B; CJ 91B; CJ91B;

IUPAC/Chemical Name

sodium (E)-5,5'-(diazene-1,2-diyl)bis(2-hydroxybenzoate)

InChi Key

ZJEFYLVGGFISGT-VRZXRVJBSA-L

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/b16-15+;;

SMILES Code

O=C([O-])C1=C(O)C=CC(/N=N/C2=CC(C([O-])=O)=C(O)C=C2)=C1.[Na+].[Na+]

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Olsalazine Disodium is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.

In vitro activity:

This study investigated the effects of olsalazine on cell proliferation and DNA methylation using canine lymphoid tumor cell lines (CLBL-1, GL-1, and UL-1). Treatment with olsalazine led to significant cell growth inhibition and increased the apoptotic rate in all three cell lines. Treatment with olsalazine reduced the total amount of 5-methylcytosine in genomic DNA, as assessed by enzyme-linked immunosorbent assay. Genome-wide analysis of DNA methylation revealed that 1,801 to 5,626 CpG sites showed decreased DNA methylation levels in three cell lines, including the promoter regions of ADAM23, FES, and CREB3L1 genes. Reference: Pol J Vet Sci. 2021 Dec;24(4):515-523. https://pubmed.ncbi.nlm.nih.gov/35179837/

In vivo activity:

The results showed that administration of olsalazine sodium 5.0 mg/kg decreased the levels of serum urate in hyperuricemic rats, and noticeably improved the fractional excretion of urate and urate clearance, exhibiting an uricosuric action. Moreover, olsalazine sodium (2.5, 5.0, 10.0 mg/kg) reduced the level of blood urea nitrogen in rats. Further study showed that olsalazine sodium reduced the mRNA expression of urate reabsorptive transporter glucose transporter 9 (GLUT9), increased the mRNA expression of urate secretory transporters, organic anion transporter 1 (OAT1), OAT3 and type 1 sodium-dependent phosphate transporter (NPT1) as well as the protein expression of OAT3 in the kidney in hyperuricemic mice. Reference: Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. https://pubmed.ncbi.nlm.nih.gov/32863294/

	Solvent	mg/mL	mM
Solubility
	DMSO	20.0	57.80
	PBS (pH 7.2)	2.0	5.78
	Water	50.0	144.50

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 346.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Itoh S, Yamazaki J, Iwahana M, Tsukamoto A. Olsalazine inhibits cell proliferation and DNA methylation in canine lymphoid tumor cell lines. Pol J Vet Sci. 2021 Dec;24(4):515-523. doi: 10.24425/pjvs.2021.139976. PMID: 35179837. 2. Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L. Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. PMID: 32863294.

In vitro protocol:

In vivo protocol:

1. Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L. Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. PMID: 32863294.

1: Niu Y, Yang P, Li H, Li Q, Lin H, Gao L, Li L. Olsalazine Sodium Increases Renal Urate Excretion by Modulating Urate Transporters in Hyperuricemic Animals. Biol Pharm Bull. 2020 Nov 1;43(11):1653-1659. doi: 10.1248/bpb.b20-00362. Epub 2020 Aug 28. PMID: 32863294. 2: Niu Y, Li H, Gao L, Lin H, Kung H, Lin MC, Leung KS, Wong MH, Xiong W, Li L. Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activity. J Pharmacol Sci. 2017 Nov;135(3):114-120. doi: 10.1016/j.jphs.2017.10.007. Epub 2017 Oct 31. PMID: 29132796. 3: Banda J, Lakshmanan R, Katepalli RB, Reddy Venati UK, Koppula R, Shiva Prasad VVS. Determination of mesalazine, a low bioavailability olsalazine metabolite in human plasma by UHPLC-MS/MS: Application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Jan 1;1008:1-10. doi: 10.1016/j.jchromb.2015.11.001. Epub 2015 Nov 4. PMID: 26606108. 4: Russo L, Schneider G, Gardiner MH, Lanes S, Streck P, Rosen S. Role of pharmacoepidemiology studies in addressing pharmacovigilance questions: a case example of pancreatitis risk among ulcerative colitis patients using mesalazine. Eur J Clin Pharmacol. 2014 Jun;70(6):709-17. doi: 10.1007/s00228-014-1660-7. Epub 2014 Mar 11. PMID: 24609467; PMCID: PMC4025187. 5: Qureshi AI, Cohen RD. Mesalamine delivery systems: do they really make much difference? Adv Drug Deliv Rev. 2005 Jan 6;57(2):281-302. doi: 10.1016/j.addr.2004.08.008. PMID: 15555743. 6: Jiang XL, Cui HF. Different therapy for different types of ulcerative colitis in China. World J Gastroenterol. 2004 May 15;10(10):1513-20. doi: 10.3748/wjg.v10.i10.1513. PMID: 15133864; PMCID: PMC4656295. 7: Knoll U, Strauhs P, Schusser G, Ungemach FR. Study of the plasma pharmacokinetics and faecal excretion of the prodrug olsalazine and its metabolites after oral administration to horses. J Vet Pharmacol Ther. 2002 Apr;25(2):135-43. doi: 10.1046/j.1365-2885.2002.00395.x. PMID: 12000534. 8: Uslu B, Yilmaz S, Ozkan SA. Determination of olsalazine sodium in pharmaceuticals by differential pulse voltammetry. Pharmazie. 2001 Aug;56(8):629-32. PMID: 11534339. 9: Kruis W, Brandes JW, Schreiber S, Theuer D, Krakamp B, Schütz E, Otto P, Lorenz-Mayer H, Ewe K, Judmaier G. Olsalazine versus mesalazine in the treatment of mild to moderate ulcerative colitis. Aliment Pharmacol Ther. 1998 Aug;12(8):707-15. doi: 10.1046/j.1365-2036.1998.00360.x. PMID: 9726382. 10: Ferry GD, Kirschner BS, Grand RJ, Issenman RM, Griffiths AM, Vanderhoof JA, Fiedorek SC, Winter HS, Hassall EG, Watkins JB, et al. Olsalazine versus sulfasalazine in mild to moderate childhood ulcerative colitis: results of the Pediatric Gastroenterology Collaborative Research Group Clinical Trial. J Pediatr Gastroenterol Nutr. 1993 Jul;17(1):32-8. doi: 10.1097/00005176-199307000-00005. PMID: 8102399. 11: Doman DB, Baum MD. Olsalazine sodium can cause myopia that can be clinically confused with the uveitis of inflammatory bowel disease. Am J Gastroenterol. 1992 Nov;87(11):1684-5. PMID: 1442711. 12: Butt JH. Outpatient management of inflammatory bowel disease. Let's keep it as simple as possible. Postgrad Med. 1992 Nov 1;92(6):69-72, 77-8, 81-4, 91-2, 94 passim. doi: 10.1080/00325481.1992.11701512. PMID: 1359520. 13: Swartz ML. Dipentum (olsalazine sodium). Gastroenterol Nurs. 1991 Dec;14(3):144-7. PMID: 1760451. 14: Wadworth AN, Fitton A. Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease. Drugs. 1991 Apr;41(4):647-64. doi: 10.2165/00003495-199141040-00009. PMID: 1711964. 15: Odlind B, Eriksson O. Olsalazine sodium stimulates chloride transport across the bullfrog cornea. Acta Physiol Scand. 1990 May;139(1):241-2. doi: 10.1111/j.1748-1716.1990.tb08917.x. PMID: 2356752. 16: Ryde EM, Ahnfelt NO. The pharmacokinetics of olsalazine sodium in healthy volunteers after a single i.v. dose and after oral doses with and without food. Eur J Clin Pharmacol. 1988;34(5):481-8. doi: 10.1007/BF01046706. PMID: 3203708. 17: Meyers S, Sachar DB, Present DH, Janowitz HD. Olsalazine sodium in the treatment of ulcerative colitis among patients intolerant of sulfasalazine. A prospective, randomized, placebo-controlled, double-blind, dose-ranging clinical trial. Gastroenterology. 1987 Dec;93(6):1255-62. doi: 10.1016/0016-5085(87)90253-8. PMID: 2890550. 18: Ryde M, Gustavsson S. Biliary excretion of olsalazine sodium in humans. Eur J Drug Metab Pharmacokinet. 1987 Jan-Mar;12(1):17-24. doi: 10.1007/BF03189857. PMID: 3609069. 19: Ryde M, Gustavsson S. Effect of olsalazine sodium on migrating motor complexes in the upper small bowel of human volunteers. Ups J Med Sci. 1987;92(3):243-51. doi: 10.3109/03009738709178694. PMID: 3448800.