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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.51%
- No. CAS: 1186229-95-7
- Fòrmula: C24H29N3O3
- Peso molecular:407.51
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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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 |
|---|---|---|---|---|
| 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.
Chemical Information
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No. CAS 1186229-95-7
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Appearance Solid
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Peso molecular 407.51
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 Related Classifications
HY-118363 Related Classifications
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