Emedastine Difumarate - CAS 87233-62-3
Catalog number:
87233-62-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H34N4O9
Molecular Weight:
534.56
COA:
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Targets:
Histamine Receptor
Description:
Emedastine is a H1 receptor antagonist. It is a second generation antihistamine. Emedastine can block the action of histamine that causes allergic symptoms. It can be used in eye drops to alleviate the symptoms of allergic conjunctivitis.
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Purity:
95%
Appearance:
Powder
Synonyms:
Emedastine fumarate; Rapimine; AL-3432A; DSSTox_CID_26911; KB 2413; KB-2413; KG 2413; KG-2413; Emadine; 1-(2-Ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole Difumarat
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Allergic conjunctivitis; Allergic rhinitis; Atopic dermatitis; Dermatitis; Urticaria
Quality Standard:
USP
Shelf Life:
2 month in rt, long tim
Quantity:
Milligrams-Grams
InChIKey:
FWLKKPKZQYVAFR-LVEZLNDCSA-N
InChI:
1S/C17H26N4O.2C4H4O4/c1-3-22-14-13-21-16-8-5-4-7-15(16)18-17(21)20-10-6-9-19(2)11-12-20;2*5-3(6)1-2-4(7)8/h4-5,7-8H,3,6,9-14H2,1-2H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1+
Canonical SMILES:
CCOCCn1c(nc2ccccc12)N3CCCN(C)CC3.OC(=O)\C=C\C(=O)O.OC(=O)\C=C\C(=O)O
Current Developer:
Alcon
1.Onset and duration of action of ketotifen 0.025% and emedastine 0.05% in seasonal allergic conjunctivitis : efficacy after repeated pollen challenges in the vienna challenge chamber.
Horak F1, Stübner P, Zieglmayer R, Kawina A, Moser M, Lanz R. Clin Drug Investig. 2003;23(5):329-37.
OBJECTIVE: To compare the efficacy, onset and duration of action, and the safety of ketotifen fumarate 0.025% ophthalmic solution and emedastine difumarate 0.05% ophthalmic solution in subjects with seasonal allergic conjunctivitis (SAC) induced by allergen exposure, using the Vienna Challenge Chamber model.
2.Efficacy of olopatadine HCI 0.1%, ketotifen fumarate 0.025%, epinastine HCI 0.05%, emedastine 0.05% and fluorometholone acetate 0.1% ophthalmic solutions for seasonal allergic conjunctivitis: a placebo-controlled environmental trial.
Borazan M1, Karalezli A, Akova YA, Akman A, Kiyici H, Erbek SS. Acta Ophthalmol. 2009 Aug;87(5):549-54. doi: 10.1111/j.1755-3768.2008.01265.x. Epub 2008 Jul 9.
PURPOSE: We aimed to compare the clinical efficacy and ocular surface variables of olopatadine, ketotifen fumarate, epinastine, emedastine and fluorometholone acetate ophthalmic solutions in preventing the signs and symptoms of seasonal allergic conjunctivitis (SAC).
3.Randomized, double-masked, placebo-controlled comparison of the efficacy of emedastine difumarate 0.05% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution in the human conjunctival allergen challenge model.
D'Arienzo PA1, Leonardi A, Bensch G. Clin Ther. 2002 Mar;24(3):409-16.
BACKGROUND: Emedastine difumarate 0.05% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution are 2 topical antiallergic agents available in the United States and other countries. Emedastine is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis. Ketotifen is indicated for the temporary relief of ocular itching caused by allergic conjunctivitis.
4.[Anti-allergic effects of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole fumarate (KB-2413)].
Saito T, Nishimura N, Tajima S, Fukuda T, Ito K. Nihon Yakurigaku Zasshi. 1987 Feb;89(2):55-62.
The effects of KB-2413 on four types of allergic reactions classified by Coombs and Gell were investigated. KB-2413 inhibited homologous passive cutaneous anaphylaxis and passive anaphylactic bronchoconstriction in guinea pigs mediated by IgE-like antibody, and ED50 values were 0.0017 mg/kg, p.o., and 0.022 mg/kg, p.o., respectively. KB-2413 also inhibited IgG-mediated anaphylactic bronchoconstriction in guinea pigs actively sensitized with egg albumin. Both complement-dependent immune hemolysis and complement-independent hypotonic hemolysis were inhibited by KB-2413 in a concentration-dependent manner. KB-2413 had no effect on the Forssman systemic reaction. The passive Arthus reaction in guinea pigs sensitized with anti-egg albumin rabbit serum was unaffected by KB-2413. However, the early stage of the active Arthus reaction in rabbits sensitized with egg albumin was inhibited. KB-2413 had an inhibitory effect on the efferent phase of delayed-type hypersensitivity induced by picryl chloride (PC-DTH) in mice.
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CAS 87233-62-3 Emedastine Difumarate

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