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阿卡他定 /Alcaftadine {[allProObj[0].p_purity_real_show]}

货号:A717146 同义名: R89674;Lastacaft

Alcaftadine is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines.

Alcaftadine 化学结构 CAS号:147084-10-4
Alcaftadine 化学结构
CAS号:147084-10-4
Alcaftadine 3D分子结构
CAS号:147084-10-4
Alcaftadine 化学结构 CAS号:147084-10-4
Alcaftadine 3D分子结构 CAS号:147084-10-4
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Alcaftadine 纯度/质量文件 产品仅供科研

货号:A717146 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Alcaftadine 生物活性

靶点
  • H2 receptor

    H2 receptor, pKi:7.2

  • H1 receptor

    H1 receptor, pKi:8.5

描述 Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. It also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects. Alcaftadine was more effective than placebo and at least as effective as olopatadine 0.01% in preventing ocular itching at 15 minutes and at 16 hours after administration[3]. Over a range of formulations and concentrations (0.05%-0.5%), alcaftadine was well tolerated and subjects reported little or no discomfort or taste perversion in any treatment group. Topical administration of alcaftadine 0.25% ophthalmic solution was well tolerated and had an acceptable safety profile[4]. Once-daily alcaftadine 0.25% ophthalmic solution demonstrated greater efficacy in prevention of ocular itching compared with olopatadine 0.2% at 3 min post-CAC (conjunctival allergen challenge) (primary endpoint), and over all time points, 16 h post-treatment instillation. Alcaftadine and olopatadine both provided effective relief compared with placebo and were generally well tolerated[5].

Alcaftadine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01390961 Allergic Conjunctivitis Phase 4 Unknown January 2012 United States, California ... 展开 >> Milton M. Hom, OD, FAAO. Azusa, California, United States, 91702 收起 <<
NCT00889330 Allergic Conjunctivitis Phase 3 Completed - United States, Ohio ... 展开 >> Fairfield, Ohio, United States Mason, Ohio, United States 收起 <<
NCT00889330 - Completed - -

Alcaftadine 参考文献

[1]Mahvan TD, Buckley WA, et al. Alcaftadine for the prevention of itching associated with allergic conjunctivitis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1025-32.

[2]Namdar R, Valdez C. Alcaftadine: a topical antihistamine for use in allergic conjunctivitis. Drugs Today (Barc). 2011 Dec;47(12):883-90.

[3]Namdar R, Valdez C. Alcaftadine: a topical antihistamine for use in allergic conjunctivitis. Drugs Today (Barc). 2011 Dec;47(12):883-90

[4]Bohets H, McGowan C, Mannens G, Schroeder N, Edwards-Swanson K, Shapiro A. Clinical pharmacology of alcaftadine, a novel antihistamine for the prevention of allergic conjunctivitis. J Ocul Pharmacol Ther. 2011 Apr;27(2):187-95

[5]McLaurin EB, Marsico NP, Ackerman SL, Ciolino JB, Williams JM, Villanueva L, Hollander DA. Ocular itch relief with alcaftadine 0.25% versus olopatadine 0.2% in allergic conjunctivitis: pooled analysis of two multicenter randomized clinical trials. Adv Ther. 2014 Oct;31(10):1059-71

Alcaftadine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL

Alcaftadine 技术信息

CAS号147084-10-4
分子式C19H21N3O
分子量 307.389
别名 R89674;Lastacaft;trade name: Lastacaft
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 40 mg/mL(130.13 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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