Lodoxamide is a potent agonist of GPR35 with an EC50 value of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor. It inhibits histamine release induced by compound 48/80 (Item No. 22173), anti-IgE, or A23187 (Item No. 11016) in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM) and inhibits A23187-induced calcium influx in mast cells. It reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml. Lodoxamine (0.1 and 10%, w/v) reduces the immediate hypersensitivity response in rat conjunctiva in vivo in a dose-dependent manner and reduces mast cell degranulation in a topical ovalbumin challenge. Formulations containing lodoxamide have been used in the treatment of vernal conjunctivitis and keratitis.
Chemical Formula: C11H6ClN3O6
Exact Mass: 310.9945
Molecular Weight: 311.63
Elemental Analysis: C, 42.40; H, 1.94; Cl, 11.38; N, 13.48; O, 30.80
InChi Code: InChI=1S/C11H6ClN3O6/c12-7-5(14-8(16)10(18)19)1-4(3-13)2-6(7)15-9(17)11(20)21/h1-2H,(H,14,16)(H,15,17)(H,18,19)(H,20,21)
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
Shelf Life: >3 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: 2934.99.03.00
Lodoxamide inhibits compound 48/80-induced histamine release and ionophore-induced 45Ca influx with associated histamine release in purified rat peritoneal mast cells. The chemotactic response of eosinophils to fMLP as well as to IL-5 is significant and dose-dependent inhibited by Lodoxamide. Lodoxamide is also able to strongly inhibit the release of eosinophil peroxidase after IgA-dependent activation and, to a lesser extent, the release of eosinophil cationic protein and eosinophil-derived neurotoxin.
Lodoxamide has been demonstrated to have cromolyn-like activity when studied in the rat peritoneal mast cell assay (PCA) model3 and in Ascaris antigen-sensitized rhesus monkeys. When given intravenously, orally, or intrabronchially by aerosol, lodoxamide significantly inhibits the increased respiratory frequency and decreased tidal volume induced by antigen challenge in Ascaris-sensitized. anesthetized rhesus monkeys. Addition of lodoxamide tromethamine to Euro-Collins or University of Wisconsin solution results in a marked decrease in lung reperfusion injury as demonstrated by increased oxygenation, decreased microvascular permeability, and increased compliance. Patients treated with lodoxamide tromethamine demonstrate an improvement in daytime breathing difficulty, cough, sputum production, and sleep.
MacKenzie AE, Caltabiano G, Kent TC, Jenkins L, McCallum JE, Hudson BD, Nicklin SA, Fawcett L, Markwick R, Charlton SJ, Milligan G. The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35. Mol Pharmacol. 2014 Jan;85(1):91-104. doi: 10.1124/mol.113.089482. Epub 2013 Oct 10. PubMed PMID: 24113750; PubMed Central PMCID: PMC3868900.
Das D, Khan M, Gul A, Alam R. Safety and efficacy of lodoxamide in vernal keratoconjunctivitis. J Pak Med Assoc. 2011 Mar;61(3):239-41. PubMed PMID: 21465936.
Verin P, Allewaert R, Joyaux JC, Piozzi E, Koliopoulos J, Bloch-Michel E; Lodoxamide Study Group. Comparison of lodoxamide 0.1% ophthalmic solution and levocabastine 0.05% ophthalmic suspension in vernal keratoconjunctivitis. Eur J Ophthalmol. 2001 Apr-Jun;11(2):120-5. PubMed PMID: 11456011.
Ciprandi G, Buscaglia S, Catrullo A, Paolieri F, Riccio AM, Fiorino N, Canonica GW. Antiallergic activity of topical lodoxamide on in vivo and in vitro models. Allergy. 1996 Dec;51(12):946-51. PubMed PMID: 9020426.
Gunduz K, Ucakhan O, Budak K, Eryilmaz T, Ozkan M. Efficacy of lodoxamide 0.1% versus N-acetyl aspartyl glutamic acid 6% ophthalmic solutions in patients with vernal keratoconjunctivitis. Ophthalmic Res. 1996;28(2):80-7. PubMed PMID: 8792357.
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