KOR agonist-9
KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus.
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。
- 分子式: C36H45N3O4
- 分子量:583.76
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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]|
κ Opioid Receptor/KOR 0.0016 nM (Ki) |
κ Opioid Receptor/KOR 1.41 nM (EC50) |
μ Opioid Receptor/MOR 0.20 nM (Ki) |
δ Opioid Receptor/DOR 15.15 nM (Ki) |
体外実験
KOR agonist-9 (compound 10e) (17 h) shows significantly lower potency for β-arrestin recruitment in HTLA-KOR Tango cells (EC50 = 4912 nM) compared to cAMP inhibition, indicating G-protein biased signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
KOR agonist-9 (5-10 mg/kg; i.p.; single dose; 4 hours pretreatment) induces dose-dependent antipruritic effects in the mouse histamine-induced pruritus model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, 18~22 g)[1]
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Dosage:2; 5; 10; 15; 20 mg/kg
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Administration:i.p.; single dose; 4 hours pretreatment
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Result:Produced dose-dependent antinociceptive effects.
Showed significant antinociception observed at the 15 mg/kg dose.
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Animal Model:ICR mice (male, 18~22 g)[1]
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Dosage:5; 10 mg/kg
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Administration:i.p.; single dose; 4 hours pretreatment
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Result:Elicited dose-dependent antipruritic activity.
Showed a significant reduction in scratching bouts observed at the 10 mg/kg dose.
化学情報
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分子量 583.76
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分子式 C36H45N3O4
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SMILES
COC1=C(O2)C([C@]([C@@H]2[C@]3(OC)[C@@H](N4CCN(C(CC5=CC=CC=C5)=O)CC4)C6)(CC7)[C@@]6(CC3)C(N7CC8CC8)C9)=C9C=C1
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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)