2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Lu AE51090

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).

For research use only. We do not sell to patients.

Lu AE51090

Lu AE51090 Chemical Structure

CAS No. : 1186229-95-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Lu AE51090 Related Antibodies

Top Publications Citing Use of Products

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1].

IC50 & Target[1]

mAChR1

61 nM (EC50)

mAChR2

2200 nM (Ki)

mAChR3

7000 nM (Ki)

mAChR4

6900 nM (Ki)

mAChR5

8900 nM (Ki)

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, 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.

Lu AE51090 Related Antibodies
Parmacokinetics
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 %
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.
Molecular Weight

407.51

Formula

C24H29N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4539 mL 12.2696 mL 24.5393 mL
5 mM 0.4908 mL 2.4539 mL 4.9079 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Lu AE51090 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lu AE510901186229-95-7Lu AE 51090Lu AE-51090mAChRMuscarinic acetylcholine receptorcognitive impairment associated with schizophreniaAlzheimer’s diseaseM1 receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Lu AE51090
Cat. No.:
HY-118363
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.