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首页-小分子抑制剂&激动剂-GPCR-Histamine Receptor-Olopatadine
Olopatadine

Chemical Structure : Olopatadine

CAS No.: 113806-05-6

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

货号: 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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5 mg ¥880 In stock
10 mg ¥1280 In stock
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50 mg ¥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 337.42
分子式 C21H23NO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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