Olsalazine (Disodium)

Names

[ Name ]:
Olsalazine (Disodium)

[Synonym ]:
Azodisal sodium
3,3'-(E)-diazène-1,2-diylbis(6-hydroxybenzoate) de disodium
Benzoic acid, 3,3'-azobis[6-hydroxy-, disodium salt
Benzoic acid, 3,3'-[(E)-1,2-diazenediyl]bis[6-hydroxy-, sodium salt (1:2)
Olsalazine Sodium Salt
Dipentum
EINECS 227-975-7
Disodium 3,3'-[(E)-1,2-diazenediyl]bis(6-hydroxybenzoate)
Olsalazine disodium
Dinatrium-3,3'-(E)-diazen-1,2-diylbis(6-hydroxybenzolcarboxylat)
Disodium 3,3'-(E)-diazene-1,2-diylbis(6-hydroxybenzoate)
MFCD00013300
Olsalazine (Disodium)

Biological Activity

[Description]:

Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.Target: AntibacterialOlsalazine is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Olsalazine is potent inhibitors of human intestinal macrophages chemotaxis to LTB4 with IC50 of 0.39 mM. Olsalazine (0.4 mM) inhibits the superoxide radical production generated by phorbol myristate acetate (PMA)-activated neutrophils or by xanthine-xanthine oxidase reaction by reduction of 31% and 73%, respectively. Olsalazine inhibits tumor growth in a rodent model of colorectal cancer. In 1,2-dimethylhydrazine-treated rats, Olsalazine (25 mg/kg/day) decreases number and volume of tumors by 58.17% and 62.67%, respectively. Administration of Olsalazine induces a 1.7-fold times increase in the number of apoptotic cells, companied with a reduction of 42.4% in cell proliferation rate.

[Related Catalog]:

Signaling Pathways >> Anti-infection >> Bacterial

Research Areas >> Infection

[References]

[1]. Nielsen, O.H., H.W. Verspaget, and J. Elmgreen, Inhibition of intestinal macrophage chemotaxis to leukotriene B4 by sulphasalazine, olsalazine, and 5-aminosalicylic acid. Aliment Pharmacol Ther, 1988. 2(3): p. 203-11.

[2]. Gionchetti, P., et al., Scavenger effect of sulfasalazine, 5-aminosalicylic acid, and olsalazine on superoxide radical generation. Dig Dis Sci, 1991. 36(2): p. 174-8.

[3]. Brown, W.A., et al., 5-aminosalicyclic acid and olsalazine inhibit tumor growth in a rodent model of colorectal cancer. Dig Dis Sci, 2000. 45(8): p. 1578-84.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
557.9ºC at 760 mmHg

[ Melting Point ]:
240ºC

[ Molecular Formula ]:
C₁₄H₈N₂Na₂O₆

[ Molecular Weight ]:
346.203

[ Flash Point ]:
291.2ºC

[ Exact Mass ]:
346.017761

[ PSA ]:
145.44000

[ LogP ]:
0.24020

[ Storage condition ]:
-20°C Freezer

Safety Information

[ HS Code ]:
2928000090

Customs

[ HS Code ]: 2928000090

[ Summary ]:
2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

Articles

Treatment of ulcerative colitis with oral mesalamine: advances in drug formulation, efficacy expectations and dose response, compliance, and chemoprevention.

Rev. Gastroenterol. Disord. 6(2) , 97-105, (2006)

Sulfasalazine, olsalazine, balsalazide, delayed-release mesalamine, controlled-release mesalamine, mesalamine pellets, and Multi-Matrix System mesalamine are effective first-line therapies for the tre...

Efficacy of drugs used in the treatment of IBD and combinations thereof in acute DSS-induced colitis in mice.

Life Sci. 92(12) , 708-18, (2013)

Although acute dextran sodium sulphate (DSS)-induced colitis in mice is frequently used as a preclinical model for testing drugs involved in inflammatory bowel disease (IBD), only limited data is avai...

Study of the plasma pharmacokinetics and faecal excretion of the prodrug olsalazine and its metabolites after oral administration to horses.

J. Vet. Pharmacol. Ther. 25(2) , 135-43, (2002)

Olsalazine sodium (Dipentum*) has been used therapeutically against inflammatory bowel disease in human medicine as an alternative to sulphasalazine over the past 20 years. Bacteria in the colon split...