Cat. No.: HY-14289

Cimetidine

(Synonyms: SKF-92334)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

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.

Purity: 99.69%
CAS No.: 51481-61-9
Formula: C₁₀H₁₆N₆S
Molecular Weight:252.34

Storage:

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

Cimetidine Chemical Structure

CAS No.: 51481-61-9

Size

Price

Stock

Quantity

Sample (0.1mg)

In-stock

(In Japan)

Apply Now

Get Quote Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability Get Quote Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability

Bulk Inquiry

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

H₂ Receptor

Histamine Receptor

0.6 μM (Ki)

All Histamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
CHO	IC₅₀	1 μM 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 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]
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 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]
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]
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]
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]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 51481-61-9
Appearance Solid
Molecular Weight 252.34
Formula C₁₀H₁₆N₆S
Color White to off-white
SMILES

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

SKF-92334
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

Publications (6)

All Cell Proliferation/Viability AssayCell Migration/Invasion AssayWB

Sort by:

Journal Impact Factor

Chemosphere

Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]

2019 Jun:225:378-387. PMID: 30884299
Emerg Contam

2026 Feb 23.
Biochim Biophys Acta Mol Basis Dis

Both carvedilol and cimetidine alleviate cisplatin-induced nephrotoxicity via downregulating OCT2. [Abstract]

2025 Jun;1871(5):167754. PMID: 40044066
Exp Neurol

Inhibition of histamine receptor 3 alleviates sevoflurane-induced hypomyelination and neurobehavioral deficits. [Abstract]

2024 Dec 3:115086. PMID: 39637962
J Evol Biochem Physiol

2025 Dec 19;61(6):1706-1719.
Ann Transl Med

Cimetidine promotes STUB1-mediated degradation of tumoral FOXP3 by activating PI3K-Akt pathway in gastric cancer. [Abstract]

2020 Oct;8(20):1304. PMID: 33209884

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.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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.

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Cimetidine

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Anti-Cardiovascular Disease Compound Library

Antibacterial Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Cimetidine

All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Cimetidine Related Classifications

Cat. No.: HY-14289