产品说明书

Cimetidine

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Chemical Structure| 51481-61-9 同义名 : 西米替汀 ;SKF-92334;NSC 335308
CAS号 : 51481-61-9
货号 : A295450
分子式 : C10H16N6S
纯度 : 98%
分子量 : 252.339
MDL号 : MFCD00133296
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

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:
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].
实验方案
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

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