Gluten Exorphin A5
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 142155-24-6
- 分子式: C29H37N5O9
- 分子量:599.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Opioid Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
δ Opioid Receptor/DOR 60 μM (IC50) |
体外実験
Gluten Exorphin A5 (10-100 μg; 2-6 h) exerts no cytotoxic effect on 70% Caco-2/30% HT-29 co-cultured cells after 2 h or 6 h of incubation[3].
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.
体内実験
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.
化学情報
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CAS 番号 142155-24-6
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分子量 599.63
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分子式 C29H37N5O9
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配列
Gly-Tyr-Tyr-Pro-Thr
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シーケンスの短縮
GYYPT
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)