Famotidine (GMP)
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine 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.
For research use only. We do not sell to patients.
- CAS No.: 76824-35-6
- Formula: C8H15N7O2S3
- Molecular Weight:337.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histamine Receptor Isoforms
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Biological Activity
|
H2 Receptor 14 nM (Kd) |
ERK1 |
ERK2 |
TLR3 |
MMP-9 |
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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] |
Chemical Information
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CAS No. 76824-35-6
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Molecular Weight 337.45
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Formula C8H15N7O2S3
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SMILES
N=C(NS(=O)(N)=O)CCSCC1=CSC(NC(N)=N)=N1
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Synonyms
MK-208 (GMP)
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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)