2. Immunology/Inflammation
  3. COX
  4. Rebamipide

Rebamipide  (Synonyms: OPC12759; Proamipide)

Cat. No.: HY-B0360 Purity: 99.60%
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Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer.

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Rebamipide Chemical Structure

Rebamipide Chemical Structure

CAS No. : 90098-04-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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1 g USD 66 In-stock
5 g USD 185 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Rebamipide:

Rebamipide Related Antibodies

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COX COX-1 COX-2 COX-3

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Description

Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer[1][2].

IC50 & Target[1]

COX-2

 

In Vitro

Rebamipide (1.4, 2.7, 5.4 mM; 24 h) inhibits proliferation of gastric cancer cell[1].
? Rebamipide (5.4 mM; 30 min) activates Smad signaling pathway in AGS cells[1].
? Rebamipide (5.4 mM; 3 h) induces the expression of Cdk inhibitor p21 in AGS cells[1].

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

Rebamipide Related Antibodies

Cell Proliferation Assay[1]

Cell Line: AGS cells
Concentration: 1.4, 2.7, 5.4 mM
Incubation Time: 24 h
Result: Significant decreased in cell proliferation in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: AGS cells
Concentration: 5.4 mM
Incubation Time: 30 min or 3 h
Result: Significantly increased phosphorylation of Smad2/3 by 1.2-fold when at 30 min and formation of Smad2/3-Smad4 complex by 1.4-fold.
Upregulated expression of p21 protein by 2.5-fold when at 3 h.
In Vivo

Rebamipide (5, 15, 50 mg/kg; p.o.; once daily for 14 days) enhances the expression of COX-2 and PGE2, and protects gastric mucosa from acid-induced injury in rat gastric mucosa[2].

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

Animal Model: Specific pathogen-free male Sprague-Dawley rats (200-230 g; 7-week-old)[2].
Dosage: 5, 15, 50 mg/kg
Administration: Oral administration; once daily for 14 days.
Result: Increased the level of COX-2 immunoreactivity and PGE2 in a dose-dependent manner. (PGE2 is implicated in protection of gastric mucosa from various insults and acceleration of gastric wound healing).
Inhibited intragastric HCl administration-induced gastric mucosal bleeding and erosion.
Clinical Trial
Molecular Weight

370.79

Formula

C19H15ClN2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C(NC(C1=CC=C(Cl)C=C1)=O)CC(C2=CC=CC=C2N3)=CC3=O)=O
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
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (67.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6969 mL 13.4847 mL 26.9694 mL
5 mM 0.5394 mL 2.6969 mL 5.3939 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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 (6.74 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.74 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6969 mL 13.4847 mL 26.9694 mL 67.4236 mL
5 mM 0.5394 mL 2.6969 mL 5.3939 mL 13.4847 mL
10 mM 0.2697 mL 1.3485 mL 2.6969 mL 6.7424 mL
15 mM 0.1798 mL 0.8990 mL 1.7980 mL 4.4949 mL
20 mM 0.1348 mL 0.6742 mL 1.3485 mL 3.3712 mL
25 mM 0.1079 mL 0.5394 mL 1.0788 mL 2.6969 mL
30 mM 0.0899 mL 0.4495 mL 0.8990 mL 2.2475 mL
40 mM 0.0674 mL 0.3371 mL 0.6742 mL 1.6856 mL
50 mM 0.0539 mL 0.2697 mL 0.5394 mL 1.3485 mL
60 mM 0.0449 mL 0.2247 mL 0.4495 mL 1.1237 mL
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Rebamipide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rebamipide90098-04-7OPC12759 ProamipideOPC 12759OPC-12759COXCyclooxygenasegastric cancerPGE2COX-2mucosal protectiongastroduodenal ulcergastritisAGS cellsInhibitorinhibitorinhibit

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