Famotidine hydrochloride
Based on 7 publication(s) in Google Scholar
Famotidine hydrochloride (MK-208 hydrochloride) 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 hydrochloride inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine hydrochloride 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 hydrochloride crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine hydrochloride reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine hydrochloride can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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- CAS No.: 125193-62-6
- Formule: C8H16ClN7O2S3
- Masse moléculaire:373.91
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Famotidine hydrochloride
More- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Int J Biol Macromol. 2024 Jun;269(Pt 2):131964. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Clin Sci. 2019 Feb 12;133(3):483-495. [Abstract]
- EMBO Rep. 2022 Jun 7;23(6):e53932. [Abstract]
- Cancers (Basel). 2021 Aug 6;13(16):3978. [Abstract]
- Curr Med Sci. 2024 Dec;44(6):1071-1080. [Abstract]
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Activité biologique
Description
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H2 Receptor 14 nM (Kd) |
ERK1 |
ERK2 |
TLR3 |
MMP-9 |
In Vitro
Famotidine (50 μM; 12 h) hydrochloride 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) hydrochloride 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) hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride undergoes apical-to-basolateral transport across Caco-2 cell monolayers via a combination of saturable facilitated diffusion and non-saturable passive diffusion, with its Papp 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. Further protocols information, click here.
In Vivo
Famotidine (10-40 mg/kg; i.p.; daily; 3 days) hydrochloride 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) hydrochloride 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.
Chemical Information
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CAS No. 125193-62-6
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Masse moléculaire 373.91
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Formule C8H16ClN7O2S3
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SMILES
O=S(N)(NC(CCSCC1=CSC(NC(N)=N)=N1)=N)=O.Cl
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Synonyms
MK-208 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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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
Famotidine hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Jun;269(Pt 2):131964. [Abstract]
MBP expression of 5 mixed corpus callosum samples of naïve, vehicle- or Famotidine (10 mg/kg)-treated mice was detected by western blotting.
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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
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
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
Famotidine hydrochloride purchased from MedChemExpress. Usage Cited in: Curr Med Sci. 2024 Dec;44(6):1071-1080. [Abstract]
Effect of histamine on BNP expression in H9c2 cells.β-MHC: β-myosin heavy chain; BNP: brain natriuretic peptide; HIS: histamine; FAM: famotidine (20 μM); GSK1016790A:TRPV4 activator; HC067047: TRPV4 channel inhibitor.
Famotidine hydrochloride purchased from MedChemExpress. Usage Cited in: Curr Med Sci. 2024 Dec;44(6):1071-1080. [Abstract]
FAM: famotidine (20 μM). Effect of histamine on TRPV4 mRNA expression.
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureté et documentation
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. [Content Brief]
[2]. Malone RW, et al. COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms. Frontiers in pharmacology. 2021;12:633680. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)