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Acrivastine/阿伐斯汀 {[allProObj[0].p_purity_real_show]}

货号:A158908 同义名: BW825C; BW 0270C

Acrivastine 是一种 H1 受体拮抗剂,常用于过敏性疾病的研究。

Acrivastine/阿伐斯汀 化学结构 CAS号:87848-99-5
Acrivastine/阿伐斯汀 化学结构
CAS号:87848-99-5
Acrivastine/阿伐斯汀 3D分子结构
CAS号:87848-99-5
Acrivastine/阿伐斯汀 化学结构 CAS号:87848-99-5
Acrivastine/阿伐斯汀 3D分子结构 CAS号:87848-99-5
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Acrivastine/阿伐斯汀 纯度/质量文件 产品仅供科研

货号:A158908 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 2HCl 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 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

99%
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

99%
Azelastine HCl 98%
Epinastine HCl 99%
Levodropropizine 97%
Cyproheptadine HCl 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin HCl 99+%
Buclizine 2HCl 95%
Latrepirdine 2HCl GluR 99%
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。

Acrivastine/阿伐斯汀 生物活性

体内研究

Acrivastine, typically administered at 8 mg three times daily, is recognized as an effective and well-tolerated antihistamine for managing chronic urticaria and allergic rhinitis. It has proven to be more effective than a placebo and similarly effective as clemastine or terfenadine in treating seasonal allergic rhinitis. In dermatoses where histamine plays a pathogenetic role, acrivastine's efficacy surpasses that of a placebo and matches that of standard doses of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine, and terfenadine. Notably, acrivastine is less likely to cause drowsiness compared to clemastine, and its adverse effects are comparable to those associated with a placebo or terfenadine[1].

Both 4 mg and 8 mg doses of acrivastine significantly alleviate symptoms of seasonal allergic rhinitis, with notable improvements in symptom scores for sneezing, runny nose, and overall symptoms. The 8 mg dose additionally reduces symptom scores for watery eyes and itchy throat, affirming acrivastine's effectiveness and tolerability in treating seasonal allergic rhinitis[2].

Acrivastine/阿伐斯汀 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
NCT01732510 Atopic Dermatitis Phase 1 Terminated(The study was prema... 展开 >>turely stopped due to business reasons.) 收起 << - -
NCT01732510 - Terminated(The study was prema... 展开 >>turely stopped due to business reasons.) 收起 << - -

Acrivastine/阿伐斯汀 参考文献

[1]Brogden RN, et al. Acrivastine. A review of its pharmacological properties and therapeutic efficacy in allergic rhinitis, urticaria and related disorders. Drugs. 1991 Jun;41(6):927-40.

[2]Gibbs TG, et al. Acrivastine in two doses compared with placebo in a multicentre, parallel group study for the treatment of seasonal allergic rhinitis. Br J Clin Pract. 1989 Jan;43(1):11-4.

Acrivastine/阿伐斯汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.43mL

28.70mL

5.74mL

2.87mL

Acrivastine/阿伐斯汀 技术信息

CAS号87848-99-5
分子式C22H24N2O2
分子量 348.44
SMILES Code O=C(O)/C=C/C1=NC(/C(C2=CC=C(C)C=C2)=C/CN3CCCC3)=CC=C1
MDL No. MFCD00869830
别名 BW825C; BW 0270C; BW A825C
运输蓝冰
InChI Key PWACSDKDOHSSQD-IUTFFREVSA-N
Pubchem ID 5284514
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(143.5 mM),配合低频超声助溶,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

H2O: 1 mg/mL(2.87 mM),配合低频超声,并水浴加热至45℃助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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