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

货号:A295450 同义名: 西米替汀 / SKF-92334;NSC 335308

Cimetidine is an antagonist of histamine-2 (H2) receptor.

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Cimetidine 化学结构 CAS号:51481-61-9
Cimetidine 化学结构
CAS号:51481-61-9
Cimetidine 3D分子结构
CAS号:51481-61-9
Cimetidine 化学结构 CAS号:51481-61-9
Cimetidine 3D分子结构 CAS号:51481-61-9
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Cimetidine 纯度/质量文件 产品仅供科研

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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

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 生物活性

靶点
  • H2 receptor

描述 Cimetidine is a histamine H2 receptor blocker with Ki and IC50 values of about 0.75 and 0.85 uM, respectively. It inhibits acid release from stomach and is used for gasterointestinal diseases and could inhibit converting hydrogen peroxide (H2O2) in a non-competitive manner. Cimetidine could non-competitively inhibit the liver catalase with high affinity. Binding of cimetidine to the enzyme induced conformational alteration in the enzyme[3]. Cimetidine, an H2-receptor antagonist, has been shown to enhance a variety of immunologic functions both in vivo and in vitro because of its inhibitory effects on suppressor-cell function. Patients receiving cimetidine have been shown to exhibit enhanced cell-mediated immunity as evaluated by increased response to skin-test antigens, restoration of sensitivity following development of acquired tolerance, and increased responses of lymphocytes to mitogen stimulation[4]. The clearance (Cl) of CsA (Cyclosporine) was significantly reduced following treatment with cimetidine when compared to the Cl value obtained in the control group (15.46 versus 10.36 ml/min/kg). Cimetidine is an inhibitor of the mixed function oxidase system enzyme system, it inhibits the metabolism of CsA[5].

Cimetidine 参考文献

[1]Sprowl JA, van Doorn L, et al. Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance. Clin Pharmacol Ther. 2013 Nov;94(5):585-92.

[2]Takahashi HK, Watanabe T, et al. Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol. 2006 Aug;70(2):450-3.

[3]Jahangirvand M, Minai-Tehrani D, Yazdi F, Minai-Tehrani A, Razmi N. Binding of Cimetidine to Balb/C Mouse Liver Catalase; Kinetics and Conformational Studies. Curr Clin Pharmacol. 2016;11(1):21-7

[4]Kumar A. Cimetidine: an immunomodulator. DICP. 1990 Mar;24(3):289-95

[5]D'Souza MJ, Pollock SH, Solomon HM. Cyclosporine-cimetidine interaction. Drug Metab Dispos. 1988 Jan-Feb;16(1):57-9

Cimetidine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.96mL

0.79mL

0.40mL

19.81mL

3.96mL

1.98mL

39.63mL

7.93mL

3.96mL

Cimetidine 技术信息

CAS号51481-61-9
分子式C10H16N6S
分子量 252.339
别名 西米替汀 ;SKF-92334;NSC 335308
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 60 mg/mL(237.78 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: 2 mg/mL(7.93 mM),配合低频超声助溶

动物实验配方
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