Ebrotidine
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.
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- Pureté : 98.08%
- CAS No.: 100981-43-9
- Formule: C14H17BrN6O2S3
- Masse moléculaire:477.42
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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HY-19748
LED209Bacterial QseC Inhibitor -
HY-15538R
Ebrotidine (Standard)Reference Standard -
HY-12532
AstemizoleH1 Receptor Antagonist -
HY-B0298A
Clemastine fumarateH1 Receptor Antagonist -
HY-B0281A
Ranitidine hydrochlorideHistamine H2-Receptor Antagonist -
HY-13511A
Rupatadine FumarateDual PAF/H1 Antagonist -
HY-15541
ZaltidineHistamine Receptor Antagonist -
HY-13511AR
Rupatadine Fumarate (Standard)Dual PAF/H1 Antagonist -
HY-12532R
Astemizole (Standard)H1 Receptor Antagonist -
HY-B0281AR
Ranitidine hydrochloride (Standard)Standard of Ranitidine hydrochloride -
HY-B0298AR
Clemastine fumarate (Standard)Standard of Clemastine fumarate
Voir tous les produits spécifiques à Isoform Histamine Receptor
MoreVoir tous les produits spécifiques à Isoform TNF Receptor
More
Activité biologique
Description
IC50 & Target
[1]|
H2 Receptor |
In Vivo
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 increased6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss CD-1 SPF (male and female)[1]
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Dosage:500 mg/kg/day
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Administration:p.o. via diet; daily; 18 months
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Result:Did not alter mucosal thickness and induced no diffuse or focal ECL-cell hyperplasia.
ECL density comparable to control.
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Animal Model:Sprague-Dawley OFA (male, 8 weeks old, SPF health rating)[2]
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Dosage:500 mg/kg
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Administration:p.o.; once daily; 60 days
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Result:Did not significantly change antral G-cell density.
Cimetidine significantly increased whole-mucosa G-cell density.
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Animal Model:Sprague-Dawley (180-200 g)[3]
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Dosage:100 mg/kg
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Administration:i.g.; twice daily; 14 days
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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.
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Animal Model:Sprague-Dawley rats (250-275 g; fasted for 24 hours, water withheld 2 hours prior to experimentation)[4]
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Dosage:100 mg/kg
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Administration:i.g.; single dose; 30 minutes before Indomethacin
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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%.
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Animal Model:OFA Sprague-Dawley CD (male and female, SPF)[5]
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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
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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
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Result:NOAEL 150 mg/kg/day.
No drug-attributable gastric mucosal change and no carcinogenic evidence in either sex.
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Animal Model:Sprague-Dawley (180-200 g)[6]
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Dosage:100 mg/kg
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Administration:i.g.; twice daily; 13 days total (3 days pretreatment, 10 days post-lipopolysaccharide application)
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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
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CAS No. 100981-43-9
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Appearance Solid
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Masse moléculaire 477.42
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Formule C14H17BrN6O2S3
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Color White to off-white
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SMILES
O=S(C1=CC=C(Br)C=C1)(/N=C/NCCSCC2=CSC(NC(N)=N)=N2)=O
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Synonyms
FI3542
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (286 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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 |
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| 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 |
Ebrotidine Related Classifications
HY-15538 Related Classifications
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Keywords
- Ebrotidine
- 100981-43-9
- FI3542
- FI 3542
- FI-3542
- Histamine Receptor
- Interleukin Related
- TNF Receptor
- Endothelin Receptor
- indomethacin-induced gastric mucosal injury
- gastric mucosal hyperplasia
- Helicobacter pylori
- acute gastritis
- Swiss CD-1 SPF mice
- gastric acid secretion
- ECL cell
- histamine H2-receptor
- chronic gastric ulcer
- antral G-cell
- Inhibitor
- inhibitor
- inhibit