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Cimetidine sulfoxide/西咪替丁亚砜 {[allProObj[0].p_purity_real_show]}

货号:A1365596 同义名: Cimetidine sulphoxide

Cimetidine sulfoxide是Cimetidine的亚砜代谢物。Cimetidine是组胺H2受体拮抗剂,具有治疗胃溃疡和上消化道出血的潜力。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Cimetidine sulfoxide/西咪替丁亚砜 化学结构 CAS号:54237-72-8
Cimetidine sulfoxide/西咪替丁亚砜 化学结构
CAS号:54237-72-8
Cimetidine sulfoxide/西咪替丁亚砜 3D分子结构
CAS号:54237-72-8
Cimetidine sulfoxide/西咪替丁亚砜 化学结构 CAS号:54237-72-8
Cimetidine sulfoxide/西咪替丁亚砜 3D分子结构 CAS号:54237-72-8
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Cimetidine sulfoxide/西咪替丁亚砜 纯度/质量文件 产品仅供科研

货号:A1365596 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。

Cimetidine sulfoxide/西咪替丁亚砜 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/西咪替丁亚砜 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/西咪替丁亚砜 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/西咪替丁亚砜 技术信息

CAS号54237-72-8
分子式C10H16N6OS
分子量 268.34
SMILES Code N#CNC(NC)=NCCS(CC1=C(C)N=CN1)=O
MDL No. MFCD09753816
别名 Cimetidine sulphoxide
运输蓝冰
InChI Key HOJLJLYVNQFCRE-UHFFFAOYSA-N
Pubchem ID 62949
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: 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

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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