Axelopran
Axelopran (TD-1211) is an orally active opioid receptor antagonist. Axelopran binds to human μ-, δ-, and κ-opioid receptors with pKi values of 9.8, 8.8, and 9.9, respectively. Axelopran (sulfate) blocks μ-opioid receptor agonist signaling, reverses opioid-induced gastrointestinal inhibition, and inhibits agonist-induced opioid receptor G protein activation. Axelopran can be used for research on opioid-induced constipation.
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: 949904-48-7
- 分子式: C26H39N3O4
- 分子量:457.61
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
Other In-stock Forms of Axelopran
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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
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μ Opioid Receptor/MOR |
κ Opioid Receptor/KOR |
δ Opioid Receptor/DOR |
体外実験
Axelopran acts as a potent antagonist in agonist-induced GTPγS binding assays at recombinant μ, δ, and κ opioid receptors (pKb = 9.6, 8.8, and 9.5, respectively)[1].
Axelopran is a P-gp substrate in Caco-2 and MDR1-MDCK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Axelopran (0.24 mg/kg; p.o.) reverses Loperamide (HY-156131)-induced delayed gastric emptying in rats[1].
Axelopran (0.01 mg/kg; p.o.) inhibits Castor oil (HY-107799)-induced diarrhea in rats[1].
Axelopran (3 mg/kg) inhibits non-productive gastrointestinal circular smooth muscle contractility in dogs[1].
Axelopran (0.03-10 mg/kg; p.o.; single administration) reverses Loperamide-induced delayed gastric emptying in rats, with an oral ED50 of 0.24 mg/kg[2].
Axelopran (0.001-0.3 mg/kg; p.o.; single administration) reverses loperamide-induced antidiarrheal activity in the rat Castor oil model, with an oral ED50 of 0.01 mg/kg[2].
Axelopran (0.03-3 mg/kg; p.o.; single administration) attenuates Loperamide-induced gastrointestinal hypermotility in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat[1]
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Dosage:ID50 0.24 mg/kg
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Administration:p.o.
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Result:Reversed loperamide-induced delay in gastric emptying with an ID50 of 0.24 mg/kg.
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Animal Model:Rat[1]
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Dosage:ID50 0.01 mg/kg
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Administration:p.o.
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Result:Inhibited castor oil-induced diarrhea with an ID50 of 0.01 mg/kg.
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Animal Model:Sprague-Dawley (male, 150-350 g)[2]
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Dosage:0.03-10 mg/kg
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Administration:p.o.; single dose
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Result:Produced dose-dependent reversal of loperamide-induced inhibition of gastric emptying.
The oral dose producing 50% reversal was 0.24 mg/kg.
The hot plate/gastric emptying peripheral selectivity index was >250.
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Animal Model:Sprague-Dawley (male, 150-350 g)[2]
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Dosage:0.001-0.3 mg/kg
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Administration:p.o.; single dose
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Result:Produced dose-dependent reversal of loperamide’s antidiarrheal activity.
The oral dose producing 50% reversal was 0.01 mg/kg.
The hot plate/castor oil peripheral selectivity index was >6,000.
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Animal Model:Beagle (female, 6.5-8.5 kg)[2]
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Dosage:0.03, 0.3, and 3 mg/kg
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Administration:p.o.; single dose
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Result:Attenuated Loperamide-induced increased contractility in the antrum, duodenum, and jejunum.
The inhibitory effect was dose-dependent.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 949904-48-7
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分子量 457.61
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分子式 C26H39N3O4
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SMILES
O=C([C@@H](O)CO)N(CC1CCCCC1)CCN2[C@H]3C[C@H](C4=CC(C(N)=O)=CC=C4)C[C@@H]2CC3
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別名
TD-1211
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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)
Axelopran 関連分類
HY-16765 関連分類
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