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Olopatadine

Chemical Structure : Olopatadine

CAS No.: 113806-05-6

Olopatadine (AL-4943A, ALO4943A, KW4679, KW-4679)

Catalog No.: PC-28136Not For Human Use, Lab Use Only.

Olopatadine (AL-4943A, KW-4679) is an antiallergic/antihistaminic agent that inhibits mast cell mediator release and possesses histamine H1 receptor (H1R) antagonist activity with Ki of 31.6 nM, shows much lower affinities for H2 receptors and H3 receptors (Ki>50 uM).

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Biological Activity

Olopatadine (AL-4943A, KW-4679) is an antiallergic/antihistaminic agent that inhibits mast cell mediator release and possesses histamine H1 receptor (H1R) antagonist activity with Ki of 31.6 nM, shows much lower affinities for H2 receptors and H3 receptors (Ki>50 uM).
Olopatadine (AL-4943A, KW-4679) inhibits histamine release in a concentration-dependent fashion (IC50 = 559 uM) from human conjunctival mast cell preparations in vitro.
Olopatadine inhibits histamine-induced phosphoinositide turnover in human conjunctival epithelial cells (IC50 = 10 nM), exhibits apparent noncompetitive antagonist properties with an estimated dissociation constant (Kb) of 19.9 nM.
Olopatadine (AL-4943A, KW-4679) effectively inhibits antigen- and histamine-stimulated conjunctivitis in guinea pigs.

Physicochemical Properties

M.Wt 337.42
Formula C21H23NO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-2-(11-(3-(Dimethylamino)propylidene)-6,11-dihydrodibenzo[b,e]oxepin-2-yl)acetic acid

References

1. Ohshima E, et al. J Med Chem. 1992 May 29;35(11):2074-84.

2. Ohshima E, et al. Chem Pharm Bull (Tokyo). 1992 Sep;40(9):2552-4.

3. Miki I, et al. Cell Immunol. 1996 Aug 1;171(2):285-8.

4. Sharif NA, et al. J Pharmacol Exp Ther. 1996 Sep;278(3):1252-61.

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