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。
HazMat Fee + 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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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. |
| 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 |
| 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 |
|
| 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 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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