Cat. No.: HY-118363

Lu AE51090

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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).

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Pureté: 99.51%
CAS No.: 1186229-95-7
Formule: C₂₄H₂₉N₃O₃
Masse moléculaire:407.51

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Lu AE51090 Chemical Structure

CAS No.: 1186229-95-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

mAChR1

61 nM (EC₅₀)

mAChR2

2200 nM (Ki)

mAChR3

7000 nM (Ki)

mAChR4

6900 nM (Ki)

mAChR5

8900 nM (Ki)

Voir tous les produits spécifiques à Isoform mAChR :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	20 μM Compound: 4, Lu AE51090	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	[PMID: 22677319]
CHO-K1	EC₅₀	61 nM Compound: 17	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	[PMID: 20684563]
CHO-K1	EC₅₀	61 nM Compound: 4, Lu AE51090	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	[PMID: 22677319]
CHO-K1	EC₅₀	97 nM Compound: 17	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	[PMID: 20684563]

In Vitro

Lu AE51090 (up to 10 μM) exhibits agonistic activity at human M1 receptor (EC₅₀ = 61 nM, E_max = 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.

Parmacokinetics

Species	Dose	Route	CL	T_1/2	V_ss	F
Rat^[1]	1 mg/kg	i.v.	5 L/h/kg	0.8 h	4.8 L/kg	4.0 %

In Vivo

Lu AE51090 (0.31-20 mg/kg, s.c., once, 30 min pre-experiment) exerts dose-dependent procognitive effects in male C57Bl/6J mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57Bl/6J mice (22-24 g)^[1]
Dosage:

0.31, 1.3, 10, 20 mg/kg
Administration:

s.c., once, 30 min pre-experiment
Result:

Achieved dose-dependent reversal of delay-induced memory decay.

Chemical Information

CAS No. 1186229-95-7
Appearance Solid
Masse moléculaire 407.51
Formule C₂₄H₂₉N₃O₃
Color White to off-white
SMILES

O=C(NC1CCN(CCCN2C3=CC=CC=C3OCC2=O)CC1)CC4=CC=CC=C4
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4539 mL

12.2696 mL

24.5393 mL

5 mM

0.4908 mL

2.4539 mL

4.9079 mL

10 mM

0.2454 mL

1.2270 mL

2.4539 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Sams AG, et al. Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. J Med Chem. 2010 Sep 9;53(17):6386-97. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Lu AE51090

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform mAChR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lu AE51090

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform mAChR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lu AE51090 Related Classifications

HY-118363 Related Classifications