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/ 组胺受体 / Roxatidine Acetate HCl

盐酸罗沙替丁醋酸酯 /Roxatidine Acetate HCl {[allProObj[0].p_purity_real_show]}

货号：A584050 同义名： HOE 760;Roxatidine Acetate (hydrochloride)

Roxatidine Acetate HCl是一种选择性组胺 H2 受体拮抗剂，IC50 为 3.2 μM，常用于胃酸分泌的抑制及溃疡相关研究。

Roxatidine Acetate HCl 化学结构 CAS号：93793-83-0
Roxatidine Acetate HCl 化学结构
CAS号：93793-83-0
Roxatidine Acetate HCl 3D分子结构
CAS号：93793-83-0
Roxatidine Acetate HCl 化学结构 CAS号：93793-83-0
Roxatidine Acetate HCl 3D分子结构 CAS号：93793-83-0
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Roxatidine Acetate HCl 纯度/质量文件 产品仅供科研

货号：A584050 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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

 		99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine hydrochloride ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin hydrochloride ✔ 99+%
Buclizine 2HCl ✔ 97%
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。

Roxatidine Acetate HCl 生物活性

靶点

  • H2 receptor

    Histamine H2 receptor, IC50:3.2 μM
描述 Roxatidine Acetate Hydrochloride is a specific and competitive H2-receptor antagonist. Roxatidine acetate and its main metabolite roxatidine inhibit histamine-induced gastric acid secretion in vitro with a potency greater than that of cimetidine, and in the range of that produced by ranitidine. In rats single or repeated dosing with roxatidine acetate did not influence drug metabolising enzymes in the liver nor did the drug show antiandrogenic activity in long term animal studies[3]. Human pharmacology studies and short-term and long-term clinical trials have all shown that roxatidine acetate is an exceptionally well tolerated compound, without the antiandrogenic activity and interference with hepatic drug metabolism which have characterized cimetidine treatment[4]. The pharmacodynamic and clinical data indicate that the efficacy of roxatidine acetate 75 mg twice-daily (b.i.d.) does not differ significantly from ranitidine 150 mg b.i.d. Roxatidine acetate is equally effective in the treatment of peptic disease including gastric ulcer, duodenal ulcer, and reflux esophagitis[5].

Roxatidine Acetate HCl 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
NCT02555852 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<

Roxatidine Acetate HCl 参考文献

[1]Pali-Scholl I, Jensen-Jarolim E. Anti-acid medication as a risk factor for food allergy. Allergy. 2011 Apr;66(4):469-77.

[2]Murdoch D, McTavish D. Roxatidine acetate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic potential in peptic ulcer disease and related disorders. Drugs. 1991 Aug;42(2):240-60.

[3]Scholtholt J, Bickel M, Herling AW. A review of the animal pharmacology of roxatidine acetate. Drugs. 1988;35 Suppl 3:30-40

[4]Dammann HG, de Looze SM, Bender W, Labs R. Clinical characteristics of roxatidine acetate: a review. Scand J Gastroenterol Suppl. 1988;146:121-34

[5]Merki HS, Bender W, Labs R. Safety and efficacy of roxatidine acetate. Evidence from pharmacodynamic and clinical trials. J Clin Gastroenterol. 1989;11 Suppl 1:S20-3; discussion S24

Roxatidine Acetate HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

12.99mL

2.60mL

1.30mL

25.98mL

5.20mL

2.60mL

Roxatidine Acetate HCl 技术信息

CAS号93793-83-0
分子式C19H29ClN2O4
分子量 384.898
别名 HOE 760;Roxatidine Acetate (hydrochloride);TZU-0460;Roxatidine Acetate Hydrochloride
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C
溶解度

DMSO: 50 mg/mL(129.9 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: 50 mg/mL(129.9 mM)
动物实验配方

Tags: Roxatidine Acetate | 93793-83-0 | HOE 760 | HOE760 | HOE-760 | Histamine H2 Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Roxatidine Acetate HCl 纯度/质量文件 | Roxatidine Acetate HCl 亚型比较 | Roxatidine Acetate HCl 生物活性 | Roxatidine Acetate HCl 临床数据 | Roxatidine Acetate HCl 参考文献 | Roxatidine Acetate HCl 实验方案 | Roxatidine Acetate HCl 技术信息

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