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

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

Cimetidine 是一种组胺 H2 受体拮抗剂(Ki = 0.6 μM),可抑制胃酸分泌,并具抗癌、抗炎活性。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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/西咪替丁 化学结构 CAS号:51481-61-9
Cimetidine/西咪替丁 化学结构
CAS号:51481-61-9
Cimetidine/西咪替丁 3D分子结构
CAS号:51481-61-9
Cimetidine/西咪替丁 化学结构 CAS号:51481-61-9
Cimetidine/西咪替丁 3D分子结构 CAS号:51481-61-9
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Cimetidine/西咪替丁 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 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 ++

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 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/西咪替丁 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/西咪替丁 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293 cells 25 µM 15 min Evaluate the inhibitory effect of Bictegravir on MATE1-mediated dofetilide transport Int J Mol Sci. 2022 Aug 3;23(15):8607.
LIM2412 1X10^-10M to 1X10^-6M 24 hours To study the effect of histamine and cimetidine on the proliferation of LIM2412 cells. Histamine significantly stimulated the proliferation of LIM2412 cells, and cimetidine antagonized this effect. Gut. 1994 Nov;35(11):1632-6.
C170 1X10^-10M to 1X10^-6M 24 hours To study the effect of histamine and cimetidine on the proliferation of C170 cells. Histamine significantly stimulated the proliferation of C170 cells, and cimetidine antagonized this effect. Gut. 1994 Nov;35(11):1632-6.
MKN45G 10^-5 M 3-4 days Cimetidine reversed histamine-stimulated proliferation of MKN45G cells but had no effect on basal growth. Gut. 1993 Aug;34(8):1091-6.
MKN45 10^-5 M 3-4 days Cimetidine reversed histamine-stimulated proliferation of MKN45 cells but had no effect on basal growth. Gut. 1993 Aug;34(8):1091-6.
Il-1β:GFP reporter cells in zebrafish larval spinal cord injury model 10µM 4 hours pre-incubation followed by 16-18 hours incubation Cimetidine significantly reduced il-1β expression and decreased inflammatory response Theranostics. 2023 Apr 23;13(8):2531-2551.
Normal rat kidney cell line (NRK) 0.1 mM 4 hours To study the protective effect of cimetidine on cisplatin-induced cytotoxicity. Cimetidine, similar to Klotho, inhibits OCT-mediated cisplatin uptake, thereby reducing cytotoxicity. Kidney Int. 2014 Apr;85(4):855-70.
SKOV-3 cells 1 mM 30 minutes Evaluate the effect of cimetidine on cisplatin uptake in SKOV-3 cells, results showed cimetidine did not affect cisplatin uptake Clin Cancer Res. 2010 Aug 15;16(16):4198-206.
293Flp-In cells 1 mM 30 minutes Evaluate the inhibitory effect of cimetidine on OCT2-mediated TEA transport, results showed cimetidine significantly inhibited OCT2 function Clin Cancer Res. 2010 Aug 15;16(16):4198-206.
A549 lung adenocarcinoma cells 500µM–3000µM 2 treatments Evaluated apoptosis by TUNEL assay, showing significant increase in apoptosis after cimetidine treatment Sci Transl Med. 2011 Aug 17;3(96):96ra77.
A549 lung adenocarcinoma cells 250µM, 500µM, 1,000µM, 1,500µM, 2,000µM 3 treatments Assessed the inhibitory effect of cimetidine on lung cancer cell growth and proliferation, showing dose-dependent inhibition Sci Transl Med. 2011 Aug 17;3(96):96ra77.

Cimetidine/西咪替丁 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Wild-type and OCT1/2 knockout mice Intravenous 30 mg/kg BW bolus followed by a maintenance infusion at a rate of 10 mg/kg/BW per h Continuous infusion for ~45 min after bolus Cimetidine significantly reduced the secretion fraction from 0.56 to 0.34 in male mice and from 0.44 to 0.23 in female mice, and significantly increased plasma creatinine levels. Kidney Int. 2010 Mar;77(6):519-26
Balb/c nu/nu mice Subcutaneous xenograft model Oral 50-200 mg/kg/day Daily administration, lasting 21-28 days To study the effect of cimetidine on the growth of C170 and LIM2412 xenografts. Cimetidine significantly inhibited tumor growth, reducing the final tumor volume of C170 to 44% of controls and LIM2412 to 60% of controls. Gut. 1994 Nov;35(11):1632-6.
Nude mice MKN45G xenograft model Drinking water 100 mg/kg/day Daily administration until the end of the experiment Cimetidine reversed histamine-stimulated growth of MKN45G xenografts and inhibited basal growth. Gut. 1993 Aug;34(8):1091-6.
SCID mice A549 lung adenocarcinoma xenograft model Intraperitoneal injection 25 mg/kg/day, 50 mg/kg/day, 100 mg/kg/day Once daily for 12 days Assessed the inhibitory effect of cimetidine on tumor growth, showing dose-dependent inhibition with the highest dose approaching the efficacy of the positive control doxorubicin Sci Transl Med. 2011 Aug 17;3(96):96ra77.
Mice Mycoplasma pneumonia model Intraperitoneal injection 40 mg/kg Daily for 7 days To evaluate the effect of cimetidine on the inflammatory response in mycoplasma pneumonia. Results showed that cimetidine significantly reduced lung inflammation and the ratio of lung weight to body weight. J Exp Med. 2006 Dec 25;203(13):2907-17
Mice Spinal cord contusion model Intraperitoneal injection 15 mg/kg Twice daily for 14 days Cimetidine significantly improved locomotor recovery in mice, reduced tissue loss, and promoted a shift towards a pro-regenerative profile of cytokine gene expression Theranostics. 2023 Apr 23;13(8):2531-2551.
Adult CD1 mice Adult mice Oral 5 mg 1-2 hours before inoculation Pretreatment with cimetidine increased gastric pH from approximately 3.0 to 3.7, preventing most of the loss of rotavirus infectivity in the adult mouse gastrointestinal tract. J Clin Invest. 1992 Jun;89(6):1741-5
Mice Oct1/2(−/−) mice Intravenous injection 30 mg/kg Single dose Evaluate the protective effect of cimetidine on cisplatin-induced nephrotoxicity, results showed cimetidine significantly reduced changes in urinary NAG activity Clin Cancer Res. 2010 Aug 15;16(16):4198-206.
Mice Yersinia enterocolitica infection model Intraperitoneal injection 20 mg/kg body weight Once daily until the conclusion of the experiment To investigate the effect of H2 receptor antagonist cimetidine on Yersinia enterocolitica infection. Results showed that cimetidine-treated mice had decreased survival and increased bacterial colonization in PPs and MLNs. Proc Natl Acad Sci U S A. 2006 Jun 13;103(24):9268-73

Cimetidine/西咪替丁 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/西咪替丁 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/西咪替丁 技术信息

CAS号51481-61-9
分子式C10H16N6S
分子量 252.34
SMILES Code CC1=C(CSCC/N=C(NC)/NC#N)NC=N1
MDL No. MFCD00133296
别名 西米替汀 ;SKF-92334; NSC 335308
运输蓝冰
InChI Key AQIXAKUUQRKLND-UHFFFAOYSA-N
Pubchem ID 2756
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

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

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
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 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
方案 一
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