Gluten Exorphin A5
Based on 1 Customer Validation
Gluten Exorphin A5 is an orally active δ-opioid receptor ligand. Gluten Exorphin A5 exhibits opioid agonist biological activity, analgesic activity, stress-induced analgesia regulatory effects, memory-promoting effects, and non-cytotoxicity. Gluten Exorphin A5 modulates intestinal permeability, can cross in vitro human intestinal epithelial cells via paracellular transport, and resists brush border peptidase hydrolysis. Gluten Exorphin A5 can be used in the research of stress-related processes and cognitive processes.
For research use only. We do not sell to patients.
- Purity : 98.79%
- CAS No.: 142155-24-6
- Formula: C29H37N5O9
- Molecular Weight:599.63
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Opioid Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
δ Opioid Receptor/DOR 60 μM (IC50) |
In Vitro
Gluten Exorphin A5 (30 μg; 30 or 120 min) passes through the 70% Caco-2/30% HT-29 intestinal epithelial co-culture layer as an intact peptide, with basolateral recovery ratios accounting for 0.5% and 3% of the apical administered dose, respectively. The Papp reaches 2.06 × 10-6 cm/s at 120 min of exposure[3].
After 2 h of incubation with Gluten Exorphin A5 (30-600 μg; 2 h), the 600 μg concentration increases the viability of 70% Caco2/30% HT-29 co-cultured cells by 20%-30%, while the 30 μg and 150 μg doses exert no significant effects[2].
Gluten Exorphin A5 (30-600 μg; 120 min) reduces the TEER of 70% Caco2/30% HT-29 co-cultured monolayers in a dose-dependent manner. After 120 min of incubation, the 600 μg dose decreases TEER by 30%, while the 30 μg dose shows no significant effect[2].
The Papp of Gluten Exorphin A5 (600 μg; 120 min) across the 70% Caco-2/30% HT-29 intestinal epithelial co-culture layer is 19.53 × 10-6 cm/s; it increases the viability of 70% Caco-2/30% HT-29 co-cultured cells by approximately 20-30%, while 30 μg and 150 μg exert no significant effects[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:70% Caco-2/30% HT-29 human colon adenocarcinoma co-culture
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Concentration:10 μg, 30 μg, 100 μg
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Incubation Time:2 h, 6 h
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Result:Cause a small, statistically non-significant decrease in cell proliferation rate after 6 h incubation compared to control values and 2 h incubation values.
Show no statistically significant differences in cell proliferation rate between different concentrations.
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Cell Line:70% Caco2/30% HT-29 co-culture cells (post-confluent day 6)
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Concentration:30 μg, 150 μg, 600 μg
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Incubation Time:2 h
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Result:Increased viability by approximately 20-30% at 600 μg; 30 and 150 μg produced no significant effect.
In Vivo
Gluten Exorphin A5 (30 or 300 μg/mouse; intracerebroventricular injection; 5 min prior to stress) inhibits foot shock stress-induced analgesia, while 300 μg/mouse enhances psychosocial stress-induced analgesia, and neither dose affects forced swimming stress-induced analgesia[1].
Gluten Exorphin A5 (30 or 300 mg/kg; p.o.; 5 min before stress) inhibits psychosocial stress-induced analgesia, but does not affect analgesia induced by foot shock or forced swimming stress[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, 22-28 g)[1]
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Dosage:30 or 300 μg/mouse
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Administration:i.c.v.
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Result:Produced mild dose-dependent antinociception, with a significant effect at 300 μg/mouse.
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Animal Model:Footshock, forced-swim and socio-psychological stress models[1]
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Dosage:30 or 300 μg/mouse
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Administration:i.c.v.; 5 min before stress
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Result:Suppressed FS-SIA; potentiated PSY-SIA at 300 μg/mouse; did not affect SW-SIA.
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Animal Model:Footshock, forced-swim and socio-psychological stress models[1]
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Dosage:30 or 300 mg/kg
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Administration:p.o.; 5 min before stress
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Result:Suppressed PSY-SIA but did not affect FS-SIA or SW-SIA.
Chemical Information
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CAS No. 142155-24-6
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Appearance Solid
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Molecular Weight 599.63
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Formula C29H37N5O9
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Sequence
Gly-Tyr-Tyr-Pro-Thr
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Sequence Shortening
GYYPT
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (166.77 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (4.17 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 (4.17 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6677 mL | 8.3385 mL | 16.6770 mL | 41.6924 mL |
| 5 mM | 0.3335 mL | 1.6677 mL | 3.3354 mL | 8.3385 mL | |
| 10 mM | 0.1668 mL | 0.8338 mL | 1.6677 mL | 4.1692 mL | |
| 15 mM | 0.1112 mL | 0.5559 mL | 1.1118 mL | 2.7795 mL | |
| 20 mM | 0.0834 mL | 0.4169 mL | 0.8338 mL | 2.0846 mL | |
| 25 mM | 0.0667 mL | 0.3335 mL | 0.6671 mL | 1.6677 mL | |
| 30 mM | 0.0556 mL | 0.2779 mL | 0.5559 mL | 1.3897 mL | |
| 40 mM | 0.0417 mL | 0.2085 mL | 0.4169 mL | 1.0423 mL | |
| 50 mM | 0.0334 mL | 0.1668 mL | 0.3335 mL | 0.8338 mL | |
| 60 mM | 0.0278 mL | 0.1390 mL | 0.2779 mL | 0.6949 mL | |
| 80 mM | 0.0208 mL | 0.1042 mL | 0.2085 mL | 0.5212 mL | |
| 100 mM | 0.0167 mL | 0.0834 mL | 0.1668 mL | 0.4169 mL |
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