Cimetidine (Synonyms: SKF-92334)

Name: Cimetidine
Brand: MedChemExpress
SKU: HY-14289
Rating: 5.0 (6 reviews)

Cat. No.: HY-14289 Purity: 99.69%: Data Sheet
COA

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Cimetidine (SKF-92334) is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a K_i of 0.6 μM. Cimetidine is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine has anti-cancer and anti-inflammatory activity.

For research use only. We do not sell to patients.

CAS No. : 51481-61-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	In-stock	Estimated Time of Arrival: December 31
50 g	Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Cimetidine:

6 Publications Citing Use of MCE Cimetidine

Cell Proliferation/Viability Assay

Cell Migration/Invasion Assay

: Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]; Our study showed that Cimetidine disrupted the proliferative capacity of GC cells by CCK8.

: Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]; Our study showed that Cimetidine (4 mM, 24 h) disrupted the proliferative capacity of GC cells byplate clone assay.

: Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]; Wound healing showed that Cimetidine (4 mM, 24 h) significantly reduced the number of migrated GC cells.

: Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]; Transwell assay showed that Cimetidine (4 mM, 24 h) significantly reduced the number of migrated GC cells.

: Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]; CCK8 assay revealed that the IC50 of Cimetidine (0-10 mM) inhibiting the viability of GC cells was increased with the decrease of FOXP3 level in these GC cells.

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

H₂ Receptor

Histamine Receptor

0.6 μM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1 x 10^-6 M Compound: Cimetidine	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	[PMID: 27876250]
CHO	IC₅₀	1 μM Compound: Cimetidine	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	[PMID: 26988801]
HEK293	IC₅₀	1.2 μM Compound: cimetidine	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	149 μM Compound: Cimetidine	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of YM155 after 1 min Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of YM155 after 1 min	[PMID: 28230985]
HRPE	IC₅₀	1.5 mM Compound: Cimetidine	TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells	[PMID: 10825452]
LLC-PK1	IC₅₀	> 50 μM Compound: Cimetidine	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Cimetidine	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Cimetidine	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells	[PMID: 12699389]
Oocyte	IC₅₀	0.59 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes	[PMID: 12176030]
Oocyte	IC₅₀	329 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 100 uM) in Xenopus laevis oocytes TP_TRANSPORTER: inhibition of TEA uptake (TEA: 100 uM) in Xenopus laevis oocytes	[PMID: 10082798]
Oocyte	IC₅₀	373 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 100 uM) in Xenopus laevis oocytes TP_TRANSPORTER: inhibition of TEA uptake (TEA: 100 uM) in Xenopus laevis oocytes	[PMID: 10082798]
Oocyte	IC₅₀	8 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes	[PMID: 12176030]
S2	IC₅₀	166 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells	[PMID: 14978359]
S2	IC₅₀	492 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells	[PMID: 14978359]
S2	IC₅₀	92.4 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells	[PMID: 14978359]
S2	IC₅₀	> 2000 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells	[PMID: 14978359]
S2	IC₅₀	> 2000 μM Compound: Cimetidine	TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in rOAT1-expressing S2 cells TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in rOAT1-expressing S2 cells	[PMID: 14978359]

In Vitro

Cimetidine (SKF-92334), a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers [1]. Cimetidine had no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells)^[3].
Cimetidine showed no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine reversed MDSC-mediated T-cell suppression, and improved IFN-γ production^[4].
Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cimetidine (SKF-92334) reduceS CD11b(+)Gr-1(+) myeloid derived-suppressive cell (MDSC) accumulation in spleen, blood and tumor tissue of tumor-bearing mice^[4].
Cimetidine exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

252.34

Formula

C₁₀H₁₆N₆S

CAS No.

51481-61-9

Appearance

Solid

Color

White to off-white

SMILES

CC1=C(CSCC/N=C(NC)/NC#N)NC=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 60 mg/mL (237.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (7.93 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.9629 mL	19.8145 mL	39.6291 mL
5 mM	0.7926 mL	3.9629 mL	7.9258 mL
10 mM	0.3963 mL	1.9815 mL	3.9629 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 3 mg/mL (11.89 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 3 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (11.89 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (11.89 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 3.12 mg/mL (12.36 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.69%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (245 KB) HNMR (139 KB) RP-HPLC (256 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. M J Smit, et al. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6802-7. [Content Brief]

[2]. Takahashi, H.K., et al., Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol, 2006. 70(2): p. 450-3. [Content Brief]

[3]. Sprowl, J.A., et al., Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance. Clin Pharmacol Ther, 2013. 94(5): p. 585-92. [Content Brief]

[4]. Zheng, Y., et al., Cimetidine suppresses lung tumor growth in mice through proapoptosis of myeloid-derived suppressor cells. Mol Immunol, 2013. 54(1): p. 74-83. [Content Brief]

[5]. Fukuda, M., K. Kusama, and H. Sakashita, Cimetidine inhibits salivary gland tumor cell adhesion to neural cells and induces apoptosis by blocking NCAM expression. BMC Cancer, 2008. 8: p. 376. [Content Brief]

[6]. Longhini, R., et al., Cimetidine Reduces the Alveolar Bone Loss in Induced Periodontitis in Rat Molars. J Periodontol, 2013. [Content Brief]

[7]. Hough LB, et al. Cimetidine penetrates brain and inhibits non-opiate footshock-induced analgesia. Pharmacol Biochem Behav. 1986 May;24(5):1257-61. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.9629 mL	19.8145 mL	39.6291 mL	99.0727 mL
H₂O / DMSO	5 mM	0.7926 mL	3.9629 mL	7.9258 mL	19.8145 mL
DMSO	10 mM	0.3963 mL	1.9815 mL	3.9629 mL	9.9073 mL
	15 mM	0.2642 mL	1.3210 mL	2.6419 mL	6.6048 mL
	20 mM	0.1981 mL	0.9907 mL	1.9815 mL	4.9536 mL
	25 mM	0.1585 mL	0.7926 mL	1.5852 mL	3.9629 mL
	30 mM	0.1321 mL	0.6605 mL	1.3210 mL	3.3024 mL
	40 mM	0.0991 mL	0.4954 mL	0.9907 mL	2.4768 mL
	50 mM	0.0793 mL	0.3963 mL	0.7926 mL	1.9815 mL
	60 mM	0.0660 mL	0.3302 mL	0.6605 mL	1.6512 mL
	80 mM	0.0495 mL	0.2477 mL	0.4954 mL	1.2384 mL
	100 mM	0.0396 mL	0.1981 mL	0.3963 mL	0.9907 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Cimetidine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cimetidine51481-61-9SKF-92334SKF92334SKF 92334Histamine ReceptorBacterialinverseanti-canceranti-inflammatoryInhibitorinhibitorinhibit

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Cimetidine (Synonyms: SKF-92334)

Customer Review

Other Forms of Cimetidine:

Cimetidine Related Antibodies

6 Publications Citing Use of MCE Cimetidine

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References

Customer Review

Cimetidine Related Antibodies

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Complete Stock Solution Preparation Table

Cimetidine Related Classifications

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