Cat. No.: HY-15538

Ebrotidine

Name: Ebrotidine
Brand: MedChemExpress
SKU: HY-15538
Price: 72.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: FI3542)

Customer Review

Based on 1 Customer Validation

Ebrotidine (FI3542) is a competitive histamine H₂ receptor (histamine H₂ receptor) antagonist with gastric acid secretion inhibitory and gastric mucosal protective effects. Ebrotidine alleviates gastric mucosal injury and epithelial cell apoptosis induced by Indomethacin (HY-14397) and Helicobacter pylori LPS (HY-D1056), and accelerates chronic gastric ulcer healing by promoting rapid recovery of IL-4 and inhibiting TNF-α, endothelin-1 (ET-1) and NOS-2. Ebrotidine can be used in studies on gastric ulcer healing, NSAID-induced gastric mucosal injury, Helicobacter pylori-associated gastritis, and H2 receptor-mediated gastric mucosal protection mechanisms.

For research use only. We do not sell to patients.

Purity : 98.08%
CAS No.: 100981-43-9
Formula: C₁₄H₁₇BrN₆O₂S₃
Molecular Weight:477.42

Storage:

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

Ebrotidine Chemical Structure

CAS No.: 100981-43-9

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

H₂ Receptor

All Histamine Receptor Isoforms :

All Interleukin Related Isoforms :

All TNF Receptor Isoforms :

All Endothelin Receptor Isoforms :

ET_A
ET_B

In Vivo

Administration of Ebrotidine (FI3542) (500 mg/kg/day; oral administration via diet; daily dosing; for 18 consecutive months) to Swiss CD-1 SPF mice does not induce gastric mucosal hyperplasia or specific ECL cell hyperplasia^[1].
Ebrotidine (500 mg/kg; p.o.; once daily; for 60 days) does not induce significant antral G cell proliferation in male Sprague-Dawley OFA rats^[2].
Ebrotidine (100 mg/kg; intragastric administration; twice daily; for 14 consecutive days) accelerates the healing of chronic gastric ulcers in Sprague-Dawley rats, achieving complete ulcer healing as early as day 7. It also promotes rapid recovery of IL-4 by day 4, rapid recovery of cNOS by day 7, accelerated reduction of TNF-α to normal levels by day 10, and reduction of ET-1 to normal levels by day 7, while downregulating the expression of caspase-3 and NOS-2 and reducing epithelial cell apoptosis^[3].
Ebrotidine (100 mg/kg; oral gavage; single administration; 30 minutes prior to indomethacin treatment) exerts a 90.2% protective effect against indomethacin-induced gastric mucosal injury. Its mechanism involves inhibiting indomethacin-triggered elevation of TNF-α by 98.3% and reducing the apoptosis rate of gastric epithelial cells by 54%^[4].
When ebrotidine (50-500 mg/kg/d; oral; daily; up to 104 weeks) is administered orally to Sprague-Dawley CD rats for 24 months, it induces no preneoplastic lesions or neoplastic effects in any examined organs or tissues, with a no-observed-adverse-effect level of 150 mg/kg/d^[5].
Ebrotidine (100 mg/kg; oral gavage; twice daily for 13 days) inhibits H. pylori lipopolysaccharide-induced gastric mucosal inflammation in rats. After 10 days of treatment, mucosal inflammation is reduced by 61.3%, epithelial cell apoptosis is decreased by 83.1%, TNFα level is lowered by 51.7%, ET-1 level is decreased by 27.6%, NOS-2 activity is reduced by 62.9%, and cNOS activity is increased^6].

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

Animal Model:

Swiss CD-1 SPF (male and female)^[1]
Dosage:

500 mg/kg/day
Administration:

p.o. via diet; daily; 18 months
Result:

Did not alter mucosal thickness and induced no diffuse or focal ECL-cell hyperplasia.
ECL density comparable to control.

Animal Model:

Sprague-Dawley OFA (male, 8 weeks old, SPF health rating)^[2]
Dosage:

500 mg/kg
Administration:

p.o.; once daily; 60 days
Result:

Did not significantly change antral G-cell density.
Cimetidine significantly increased whole-mucosa G-cell density.

Animal Model:

Sprague-Dawley (180-200 g)^[3]
Dosage:

100 mg/kg
Administration:

i.g.; twice daily; 14 days
Result:

Accelerated healing to 7 days.
IL-4 recovered by day 4, ET-1 by day 7, TNF-α/cNOS by day 10.
Reduced apoptosis and caspase-3.

Animal Model:

Sprague-Dawley rats (250-275 g; fasted for 24 hours, water withheld 2 hours prior to experimentation)^[4]
Dosage:

100 mg/kg
Administration:

i.g.; single dose; 30 minutes before Indomethacin
Result:

Blocked 98.3% of TNF-α rise.
Reduced apoptosis 54% and mucosal damage 90.2%.
Omeprazole reduced damage 64%, TNF-α 15%, apoptosis 16%.

Animal Model:

OFA Sprague-Dawley CD (male and female, SPF)^[5]
Dosage:

50 mg/kg/d; 200 mg/kg/d (first 13 months) then 150 mg/kg/d (remaining 11 months); 300 mg/kg/d (final 11 months); 500 mg/kg/d
Administration:

p.o.; daily; 104 weeks (50, 500 mg/kg/d); daily for first 13 months then daily for remaining 11 months (200/150 mg/kg/d); daily for final 11 months (300 mg/kg/d); mixed with diet
Result:

NOAEL 150 mg/kg/day.
No drug-attributable gastric mucosal change and no carcinogenic evidence in either sex.

Animal Model:

Sprague-Dawley (180-200 g)^[6]
Dosage:

100 mg/kg
Administration:

i.g.; twice daily; 13 days total (3 days pretreatment, 10 days post-lipopolysaccharide application)
Result:

At day 10 reduced inflammation 61.3%, apoptosis 83.1%, TNF-α 51.8%, ET-1 27.6%, NOS-2 62.9%.
Raised cNOS activity 78.6%.

Chemical Information

CAS No. 100981-43-9
Appearance Solid
Molecular Weight 477.42
Formula C₁₄H₁₇BrN₆O₂S₃
Color White to off-white
SMILES

O=S(C1=CC=C(Br)C=C1)(/N=C/NCCSCC2=CSC(NC(N)=N)=N2)=O
Synonyms

FI3542
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 : 100 mg/mL (209.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.0946 mL

10.4730 mL

20.9459 mL

5 mM

0.4189 mL

2.0946 mL

4.1892 mL

10 mM

0.2095 mL

1.0473 mL

2.0946 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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 (5.24 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 (5.24 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 (5.24 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

References

[1]. Romero A, et al. Study of the Population of Enterochromaffin-Like Cells in Mouse Gastric Mucosa after Long-Term Treatment with Ebrotidine. Toxicologic Pathology. 1996;24(2):160-165.

[2]. Romero A, et al. Effect of ebrotidine on the density of antral G-cells in the gastric mucosa in the rat. Cell proliferation. 1995 Jul;28(7):393-401.

[3]. Slomiany BL, et al. Involvement of interleukin-4 in down-regulation of endothelin-1 during gastric ulcer healing: Effect of ebrotidine. Inflammopharmacology. 2000;8(1):55-68.

[4]. Slomiany BL, et al. Induction of tumor necrosis factor-alpha and apoptosis in gastric mucosal injury by indomethacin: effect of omeprazole and ebrotidine. Scandinavian journal of gastroenterology. 1997 Jul;32(7):638-42.

[5]. Romero A, et al. Twenty-four-month oral carcinogenicity study of ebrotidine in rats. Teratogenesis, carcinogenesis, and mutagenesis. 1998;18(6):263-77.

[6]. Slomiany BL, et al. Effect of ebrotidine on Helicobacter pylori lipopolysaccharide-induced up-regulation of endothelin-1 in gastric mucosa. Journal of Endotoxin Research. 1999;5(5/6):279-285.

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	2.0946 mL	10.4730 mL	20.9459 mL	52.3648 mL
	5 mM	0.4189 mL	2.0946 mL	4.1892 mL	10.4730 mL
	10 mM	0.2095 mL	1.0473 mL	2.0946 mL	5.2365 mL
	15 mM	0.1396 mL	0.6982 mL	1.3964 mL	3.4910 mL
	20 mM	0.1047 mL	0.5236 mL	1.0473 mL	2.6182 mL
	25 mM	0.0838 mL	0.4189 mL	0.8378 mL	2.0946 mL
	30 mM	0.0698 mL	0.3491 mL	0.6982 mL	1.7455 mL
	40 mM	0.0524 mL	0.2618 mL	0.5236 mL	1.3091 mL
	50 mM	0.0419 mL	0.2095 mL	0.4189 mL	1.0473 mL
	60 mM	0.0349 mL	0.1745 mL	0.3491 mL	0.8727 mL
	80 mM	0.0262 mL	0.1309 mL	0.2618 mL	0.6546 mL
	100 mM	0.0209 mL	0.1047 mL	0.2095 mL	0.5236 mL

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Ebrotidine

All Histamine Receptor Isoforms

All Interleukin Related Isoforms

All TNF Receptor Isoforms

All Endothelin Receptor Isoforms