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货号:A1365596 同义名: Cimetidine sulphoxide

Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment[1].

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Cimetidine sulfoxide 化学结构 CAS号:54237-72-8
Cimetidine sulfoxide 化学结构
CAS号:54237-72-8
Cimetidine sulfoxide 3D分子结构
CAS号:54237-72-8
Cimetidine sulfoxide 化学结构 CAS号:54237-72-8
Cimetidine sulfoxide 3D分子结构 CAS号:54237-72-8
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Cimetidine sulfoxide 纯度/质量文件 产品仅供科研

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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%
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Histamine H1 receptor, IC50: 47 nM

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

Histamine H1 receptor, IC50: 3 nM

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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 99%
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。

Cimetidine sulfoxide 生物活性

描述 Cimetidine sulfoxide (Cimetidine sulphoxide) is a metabolite of Cimetidine, which is a histamine H2-receptor antagonist. Cimetidine exhibits potential for the treatment of peptic ulcer disease and upper gastrointestinal hemorrhage [1].
体内研究

The enantiomeric profile of Cimetidine sulfoxide is analyzed in rat urine collected over 24 hours after the oral administration of Cimetidine (30 mg/kg) to male Wistar rats. The resulting enantiomeric ratio is determined to be (+/−) 57:43 [3].

体外研究

Active transport of Cimetidine across the rat small intestine is evident at lower substrate concentrations (40 and 200 μM), but becomes obscured by passive transfer at higher concentrations (400 μM). Detection of Cimetidine sulfoxide occurs after certain incubation periods [2].

Cimetidine sulfoxide 参考文献

[1]Larsson R, et al. The pharmacokinetics of cimetidine and its sulphoxide metabolite in patients with normal and impaired renal function. Br J Clin Pharmacol. 1982;13(2):163-170.

[2]HE Barber, et al. The Transport of Cimetidine Across the Rat Small Intestine in Vitro. B r J Pharmacol. 1979 Jul;66(3):496P-497P.

[3]Ryta A. Kuzel, et al. Investigations into the chirality of the metabolic sulfoxidation of cimetidine. Chirality (1994), 6(8), 607-14.

Cimetidine sulfoxide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.73mL

0.75mL

0.37mL

18.63mL

3.73mL

1.86mL

37.27mL

7.45mL

3.73mL

Cimetidine sulfoxide 技术信息

CAS号54237-72-8
分子式C10H16N6OS
分子量 268.339
别名 Cimetidine sulphoxide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 85 mg/mL(316.76 mM),配合低频超声,并水浴加热至45℃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

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