Cat. No.: HY-B0377

Famotidine

(Synonyms: MK-208)

7 Cited Publications

Avis client

Based on 7 publication(s) in Google Scholar

Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

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Pureté: 99.85%
CAS No.: 76824-35-6
Formule: C₈H₁₅N₇O₂S₃
Masse moléculaire:337.45

Stockage:

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

Famotidine Chemical Structure

CAS No.: 76824-35-6

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

H₂ Receptor

14 nM (Kd)

ERK1

ERK2

TLR3

MMP-9

Voir tous les produits spécifiques à Isoform Histamine Receptor :

Voir tous les produits spécifiques à Isoform MMP :

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>300 μM Compound: famotidine	Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	0.76 μM Compound: famotidine	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	10.7 μM Compound: famotidine	Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	36.1 μM Compound: famotidine	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	36.2 μM Compound: famotidine	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
Sf21	IC₅₀	>1000 μM Compound: Famotidine	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	>1000 μM Compound: Famotidine	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]

In Vitro

Famotidine (50 μM; 12 h) inhibits Histamine (HY-B1204)-induced TLR3 mRNA expression in A549 cells without affecting TLR7 expression; it also suppresses the cumulative upregulation of TLR3 expression in A549 cells co-treated with Histamine and poly (I:C) (HY-107202)^[1].
Famotidine (50 μM; 12 h preincubation, 1 h or 12 h poly (I:C) treatment) inhibits Histamine-enhanced TLR3-dependent activation of the TBK1/IRF3 and NF-κB pathways, and reduces the expression of downstream genes in poly (I:C)-treated A549 cells^[1].
Famotidine (50 μM; 12 h preincubation, 24 h SARS-CoV-2 infection) reduces the expression of TLR3 in SARS-CoV-2-infected Caco-2 cells, inhibits the Histamine-enhanced TLR3-dependent signaling pathway, and downregulates the mRNA levels of downstream inflammatory mediators; it also exerts an inhibitory effect on the Histamine-enhanced TLR3-dependent signaling pathway in SARS-CoV-2-infected Caco-2 cells^[1].
Famotidine is a selective inverse agonist and biased arrestin partial agonist for the human histamine H₂ receptor, with a binding affinity of 14 nM, an inverse agonist potency of 33 nM, and an EC₅₀ of 105 nM for arrestin recruitment. It does not exhibit significant interactions with H₁, H₃, or H₄ receptors^[2].
Famotidine induces a concentration-dependent, saturable increase in transepithelial electrical resistance (TEER) across Caco-2 cell monolayers via interaction with paracellular anion sites rather than tight junction tightening, reaching 193% of the control group at 25 mM^[5].
Famotidine undergoes apical-to-basolateral transport across Caco-2 cell monolayers via a combination of saturable facilitated diffusion and non-saturable passive diffusion, with its P_app value decreasing exponentially with concentration; it selectively inhibits the apical-to-basolateral transport of the cationic Ranitidine (HY-B0693) across Caco-2 cell monolayers, indicating that it targets cation-selective conductance via paracellular anion sites^[5].

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

In Vivo

Famotidine (5-40 mg/kg; i.p.; single dose) exerts dose-dependent antinociceptive activity in the mouse hot plate test^[3].
Famotidine (10-40 mg/kg; i.p.; daily; 3 days) pretreatment for three consecutive days dose-dependently reduces carbon tetrachloride-induced hepatotoxicity in mice, as evidenced by significant decreases in serum ALT and ALP levels^[3].
Famotidine (10-60 mg/kg bw; p.o.; single dose; 30 min before ethanol) dose-dependently protects against ethanol-induced acute gastric ulcer in rats, and suppressing oxidative stress, inflammatory cell infiltration, and proinflammatory cytokine secretion^[4].

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

Essai clinique

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

Chemical Information

CAS No. 76824-35-6
Appearance Solid
Masse moléculaire 337.45
Formule C₈H₁₅N₇O₂S₃
Color White to off-white
SMILES

N=C(NS(=O)(N)=O)CCSCC1=CSC(NC(N)=N)=N1
Synonyms

MK-208
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (7)

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ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Int J Biol Macromol

Targeting of KOR by famotidine promotes OPC maturation differentiation and CNS remyelination via STAT3 signaling pathway. [Abstract]

2024 Jun;269(Pt 2):131964. PMID: 38692525
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Clin Sci (Lond)

Omeprazole prevents CDX2 and SOX9 expression by inhibiting hedgehog signaling in Barrett's esophagus cells. [Abstract]

2019 Feb 12;133(3):483-495. PMID: 30705106
EMBO Rep

CDK inhibitor Palbociclib targets STING to alleviate autoinflammation. [Abstract]

2022 Jun 7;23(6):e53932. PMID: 35403787
Cancers (Basel)

Drug Repurposing to Identify a Synergistic High-Order Drug Combination to Treat Sunitinib-Resistant Renal Cell Carcinoma. [Abstract]

2021 Aug 6;13(16):3978. PMID: 34439134
Curr Med Sci

Mast Cells Contribute to Pressure Overload-Induced Myocardial Hypertrophy by Upregulating TRPV4 via Histamine: Role of Ca2+/ CnA/NFATc3 Signaling Pathway. [Abstract]

2024 Dec;44(6):1071-1080. PMID: 39672998

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (296.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

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

2.9634 mL

14.8170 mL

29.6340 mL

5 mM

0.5927 mL

2.9634 mL

5.9268 mL

10 mM

0.2963 mL

1.4817 mL

2.9634 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (286 KB)
SDS (393 KB)
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- 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)
Instruction de manipulation (2659 KB)

Références

[1]. Mukherjee R, et al. Famotidine inhibits toll-like receptor 3-mediated inflammatory signaling in SARS-CoV-2 infection. The Journal of biological chemistry. 2021 Aug;297(2):100925.

[2]. Malone RW, et al. COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms. Frontiers in pharmacology. 2021;12:633680.

[3]. Ahmadi A, et al. Hepatoprotective, antinociceptive and antioxidant activities of cimetidine, ranitidine and famotidine as histamine H₂ receptor antagonists. Fundam Clin Pharmacol. 2011;25(1):72-79.

[4]. Pradeepkumar Singh L, et al. Novel role of famotidine in downregulation of matrix metalloproteinase-9 during protection of ethanol-induced acute gastric ulcer. Free radical biology & medicine. 2007 Jul 15;43(2):289-99.

[5]. Lee K, et al. Saturable transport of H2-antagonists ranitidine and famotidine across Caco-2 cell monolayers. Journal of pharmaceutical sciences. 1999 Jul;88(7):680-7.

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
DMSO	1 mM	2.9634 mL	14.8170 mL	29.6340 mL	74.0850 mL
	5 mM	0.5927 mL	2.9634 mL	5.9268 mL	14.8170 mL
	10 mM	0.2963 mL	1.4817 mL	2.9634 mL	7.4085 mL
	15 mM	0.1976 mL	0.9878 mL	1.9756 mL	4.9390 mL
	20 mM	0.1482 mL	0.7409 mL	1.4817 mL	3.7043 mL
	25 mM	0.1185 mL	0.5927 mL	1.1854 mL	2.9634 mL
	30 mM	0.0988 mL	0.4939 mL	0.9878 mL	2.4695 mL
	40 mM	0.0741 mL	0.3704 mL	0.7409 mL	1.8521 mL
	50 mM	0.0593 mL	0.2963 mL	0.5927 mL	1.4817 mL
	60 mM	0.0494 mL	0.2470 mL	0.4939 mL	1.2348 mL
	80 mM	0.0370 mL	0.1852 mL	0.3704 mL	0.9261 mL
	100 mM	0.0296 mL	0.1482 mL	0.2963 mL	0.7409 mL

Famotidine

7 Cited Publications

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Famotidine

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Publications Citing Use of MedChemExpress (MCE) Famotidine

Voir tous les produits spécifiques à Isoform Histamine Receptor

Voir tous les produits spécifiques à Isoform MMP

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR)

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Famotidine Related Classifications

HY-B0377 Related Classifications