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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。 |
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]. |
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 << | - | - |
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 |
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 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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