Lu AE51090
Based on 1 Customer Validation
Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS).
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。
- 純度: 99.51%
- CAS 番号: 1186229-95-7
- 分子式: C24H29N3O3
- 分子量:407.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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mAChR1 61 nM (EC50) |
mAChR2 2200 nM (Ki) |
mAChR3 7000 nM (Ki) |
mAChR4 6900 nM (Ki) |
mAChR5 8900 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
20 μM
Compound: 4, Lu AE51090
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Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay
Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay
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[PMID: 22677319] |
| CHO-K1 | EC50 |
61 nM
Compound: 17
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Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
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[PMID: 20684563] |
| CHO-K1 | EC50 |
61 nM
Compound: 4, Lu AE51090
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Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
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[PMID: 22677319] |
| CHO-K1 | EC50 |
97 nM
Compound: 17
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Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
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[PMID: 20684563] |
Lu AE51090 (up to 10 μM) exhibits agonistic activity at human M1 receptor (EC50 = 61 nM, Emax = 83%) in Ca2+ mobilization assays using CHO-K1/BHK-21 cells expressing respective receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | Vss | F |
|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 5 L/h/kg | 0.8 h | 4.8 L/kg | 4.0 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57Bl/6J mice (22-24 g)[1]
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Dosage:0.31, 1.3, 10, 20 mg/kg
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Administration:s.c., once, 30 min pre-experiment
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Result:Achieved dose-dependent reversal of delay-induced memory decay.
化学情報
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CAS 番号 1186229-95-7
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性状 Solid
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分子量 407.51
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分子式 C24H29N3O3
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Color White to off-white
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SMILES
O=C(NC1CCN(CCCN2C3=CC=CC=C3OCC2=O)CC1)CC4=CC=CC=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (306.74 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 2.4539 mL | 12.2696 mL | 24.5393 mL | 61.3482 mL |
| 5 mM | 0.4908 mL | 2.4539 mL | 4.9079 mL | 12.2696 mL | |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4539 mL | 6.1348 mL | |
| 15 mM | 0.1636 mL | 0.8180 mL | 1.6360 mL | 4.0899 mL | |
| 20 mM | 0.1227 mL | 0.6135 mL | 1.2270 mL | 3.0674 mL | |
| 25 mM | 0.0982 mL | 0.4908 mL | 0.9816 mL | 2.4539 mL | |
| 30 mM | 0.0818 mL | 0.4090 mL | 0.8180 mL | 2.0449 mL | |
| 40 mM | 0.0613 mL | 0.3067 mL | 0.6135 mL | 1.5337 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.2270 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0225 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3067 mL | 0.7669 mL | |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 mL |
Lu AE51090 関連分類
HY-118363 関連分類
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