Famotidine (MK208)

Alias: MK-208; MK 208; Pepcid; YM-11170; MK208; MK-208; YM11170; YM 11170
Cat No.:V1223 Purity: ≥98%
Famotidine (formerly YM-11170, MK208; MK-208, YM11170; Pepcid) is a competitive histamine H2–receptor antagonist with an IC50 of 0.6 mM.
Famotidine (MK208) Chemical Structure CAS No.: 76824-35-6
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5g
10g
Other Sizes

Other Forms of Famotidine (MK208):

  • Famotidine-13C,d3
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Famotidine (formerly YM-11170, MK208; MK-208, YM11170; Pepcid) is a competitive histamine H2–receptor antagonist with an IC50 of 0.6 mM. It is frequently used to treat heartburn, GERD, ulcers, and other digestive disorders because it inhibits the production of stomach acid. Famotidine does not appear to interact with other medications, unlike cimetidine, the first H2 antagonist, and it has no effect on the cytochrome P450 enzyme system.

Biological Activity I Assay Protocols (From Reference)
Targets
H2 receptor
ln Vitro

In vitro activity: Famotidine (MK-208) is a histamine H2-receptor antagonist that is frequently used to treat gastroesophageal reflux disease (GERD/GORD) and peptic ulcer disease (PUD). It does this by inhibiting the production of stomach acid. On both the third and seventh days following surgery, the Famotidine (MK-208) Group's equivalent parameters (2 mg/kg/day) were significantly lower than those of the Control Group. In the colon of rats, famotidine (MK-208) has a negative impact on the hydroxyproline content of perianastomotic tissues and the anastomotic bursting pressure[1]. Rats treated with acidified ethanol had a decrease in transgastric potential difference (PD), which was reversed by the administration of fumarate (MK-208). Famotidine's ability to prevent gastric lesions can be attributed to both the activation of the gastric mucosal defensive mechanisms and the suppression of acid secretion[2].

ln Vivo
Famotidine (MK-208) is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD). Famotidine (MK-208) Group(2 mg/kg/day) were significantly lower than the equivalent parameters for the Control Group on both the third and seventh days post-surgery. Famotidine (MK-208) exerts detrimental effects on the anastomotic bursting pressure and hydroxyproline content of perianastomotic tissues in the colon of rats. Famotidine (MK-208) increased the transgastric potential difference (PD) and promoted the recovery of decreased transgastric PD induced by acidified ethanol in rats. The preventive effect of famotidine on gastric lesions is attributable not only to suppression of acid secretion but to activation of the gastric mucosal defensive mechanisms.
Animal Protocol
2 mg/kg
Rats
References

[1]. Effects of the histamine H2 receptor antagonist famotidine on the healing of colonic anastomosis in rats. Clinics (Sao Paulo), 2009. 64(6): p. 567-70.

[2]. Studies on the mechanism for the gastric mucosal protection by famotidine in rats. Jpn J Pharmacol, 1991. 55(2): p. 211-22.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C8H15N7O2S3
Molecular Weight
337.45
Exact Mass
337.04
Elemental Analysis
C, 28.47; H, 4.48; N, 29.06; O, 9.48; S, 28.51
CAS #
76824-35-6
Related CAS #
Famotidine-13C,d3; 2744683-81-4
Appearance
White to off-white solid powder
SMILES
C1=C(N=C(S1)N=C(N)N)CSCC/C(=N/S(=O)(=O)N)/N
InChi Key
XUFQPHANEAPEMJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H15N7O2S3/c9-6(15-20(12,16)17)1-2-18-3-5-4-19-8(13-5)14-7(10)11/h4H,1-3H2,(H2,9,15)(H2,12,16,17)(H4,10,11,13,14)
Chemical Name
3-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]-N'-sulfamoylpropanimidamide
Synonyms
MK-208; MK 208; Pepcid; YM-11170; MK208; MK-208; YM11170; YM 11170
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~67 mg/mL (~198.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04724720 Active
Recruiting
Drug: Famotidine
Drug: Placebo
Covid-19 Northwell Health January 19, 2021 Phase 2
NCT05077332 Active
Recruiting
Drug: Famotidine
Drug: Celecoxib
Covid19
COVID-19 Pandemic
2019-nCoV Disease
Leidos Life Sciences December 29, 2021 Phase 2
NCT04724720 Active
Recruiting
Drug: Famotidine
Drug: Placebo
Covid-19 Northwell Health January 19, 2021 Phase 2
NCT05061303 Active
Recruiting
Other: Assessment of the drug
concentration in the blood
Kidney Rejection Transplant Poznan University of Medical
Sciences
October 17, 2021 N/A
NCT04614974 Active
Recruiting
Drug: Famotidine
Other: Speech Language Therapy
Laryngomalacia
Gastro Esophageal Reflux
Reema Padia November 18, 2020 Phase 1
Phase 2
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