AE9C90CB
AE9C90CB is an M3 muscarinic receptor (mAChR) antagonist and M2 muscarinic receptor ligand (human pKi values of 9.9 and 8.6, respectively). AE9C90CB binds to the M3 receptor and produces an insurmountable antagonism of Carbamoylcholine chloride (HY-B1208)-induced bladder strip contraction, thereby inhibiting the elevation of intravesical pressure and salivation, and exhibits functional selectivity for the bladder relative to the salivary glands. AE9C90CB can be used in the study of overactive bladder.
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: 893426-98-7
- 分子式: C21H25ClN2O2
- 分子量:372.89
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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]
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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
生物活性
製品説明
IC50 & Target
[1]|
mAChR3 9.9 (pKi) |
mAChR2 8.6 (pKi) |
体外実験
AE9C90CB (3 h) exhibits high affinity for human recombinant muscarinic M3 receptors (pKi 9.9) with moderate selectivity for M3 over M2 receptors in CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Urethane (1.5 g/kg, i.v.)-anaesthetized rabbit model with bladder catheterization and intravesical pressure recording, challenged with carbachol (1.5 μg/kg, i.a.)[1]
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Dosage:3 μg/kg
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Administration:Intravenous (i.v.) bolus; each dose separated by a 30-min interval
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Result:Effectively inhibited the Carbachol-induced increase in intravesical pressure, with an ED50 of 3 μg/kg; ED50 for salivation = 16 μg/kg; bladder versus salivary gland selectivity = 5.4.
化学情報
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CAS 番号 893426-98-7
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分子量 372.89
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分子式 C21H25ClN2O2
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SMILES
[H][C@@]1(CNC2)[C@@]2([H])[C@H]1CN(C)C(C(C3=CC=CC=C3)(C4=CC=CC=C4)O)=O.Cl
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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)
AE9C90CB 関連分類
HY-134971 関連分類
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