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CAS No.: 147084-10-4

Alcaftadine/阿卡他定 Catalog No. CSN10231

Synonyms: R89674;trade name: Lastacaft;阿卡他定

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

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技术信息

生物活性

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].
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 ... more >> Milton M. Hom, OD, FAAO. Azusa, California, United States, 91702 Collapse <<
NCT00889330	Allergic Conjunctivitis	Phase 3	Completed	-	United States, Ohio ... more >> Fairfield, Ohio, United States Mason, Ohio, United States Collapse <<
NCT00889330	-	-	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2532 mL
- 16.2660 mL
- 32.5320 mL
- 5 mM
- 0.6506 mL
- 3.2532 mL
- 6.5064 mL
- 10 mM
- 0.3253 mL
- 1.6266 mL
- 3.2532 mL

技术信息

CAS号

147084-10-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21N3O

运输

蓝冰

分子量

307.39

别名

R89674;trade name: Lastacaft;阿卡他定

溶解度

DMSO	160.0 mg/mL (520.5 mM)
Water	insoluble

动物实验配方

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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 ... more >> Milton M. Hom, OD, FAAO. Azusa, California, United States, 91702 Collapse <<
NCT00889330	Allergic Conjunctivitis	Phase 3	Completed	-	United States, Ohio ... more >> Fairfield, Ohio, United States Mason, Ohio, United States Collapse <<
NCT00889330	-	-	Completed	-	-
NCT02308501	Allergic Conjunctivitis	Phase 4	Completed	-	-
NCT01470118	Conjunctivitis, Allergic	Phase 4	Completed	-	United States, Pennsylvania ... more >> Philadelphia, Pennsylvania, United States Collapse <<
NCT01732757	Conjunctivitis, Allergic	Phase 4	Completed	-	United States, Tennessee ... more >> Memphis, Tennessee, United States Collapse <<
NCT01470118	-	-	Completed	-	-
NCT01339507	-	-	Completed	-	United States, Texas ... more >> Derek Cunningham Austin, Texas, United States, 78746 Collapse <<
NCT01732757	-	-	Completed	-	-
NCT02555761	-	-	Completed	-	-
NCT01808768	Allergic Conjunctivitis ... more >> Rhinoconjunctivitis Collapse <<	Phase 4	Unknown	November 2013	United States, New Jersey ... more >> STARx Research Center Recruiting Edison, New Jersey, United States, 08820 Contact: Erika Julca, lpn,crc 732-906-1747 ejulca1@gmail.com Contact: June Pepe, lpn, ccrc 973-912-9817 pepejune@gmail.com Principal Investigator: Jayesh Kanuga, MD Sub-Investigator: Ligaya Centeno, MD Sub-Investigator: Ruby Reyes, MD Sub-Investigator: Leonard Bielory, MD STARx Recruiting Springfield, New Jersey, United States, 07081 Contact: Leonard Bielory, MD 973-912-9817 DrLBielory@gmail.com Sub-Investigator: Leonard Bielory, MD Collapse <<

Alcaftadine/阿卡他定 Catalog No. CSN10231

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