Home >> Research Area >>Neuroscience>>5-HT Receptor>> Lu AE58054 Hydrochloride

Lu AE58054 Hydrochloride

5-HT(6)R antagonist CAS# 467458-02-2

Lu AE58054 Hydrochloride

Catalog No. BCC1708----Order now to get a substantial discount!

Product Name & Size Price Stock
Lu AE58054 Hydrochloride: 5mg $253 In Stock
Lu AE58054 Hydrochloride: 10mg Please Inquire In Stock
Lu AE58054 Hydrochloride: 20mg Please Inquire Please Inquire
Lu AE58054 Hydrochloride: 50mg Please Inquire Please Inquire
Lu AE58054 Hydrochloride: 100mg Please Inquire Please Inquire
Lu AE58054 Hydrochloride: 200mg Please Inquire Please Inquire
Lu AE58054 Hydrochloride: 500mg Please Inquire Please Inquire
Lu AE58054 Hydrochloride: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Lu AE58054 Hydrochloride

Number of papers citing our products

Chemical structure

Lu AE58054 Hydrochloride

3D structure

Chemical Properties of Lu AE58054 Hydrochloride

Cas No. 467458-02-2 SDF Download SDF
PubChem ID 21071391 Appearance Powder
Formula C20H20ClF5N2O M.Wt 434.83
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Idalopirdine Hydrochloride
Solubility DMSO : ≥ 25 mg/mL (57.49 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-(6-fluoro-1H-indol-3-yl)-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]ethanamine;hydrochloride
SMILES C1=CC(=CC(=C1)OCC(C(F)F)(F)F)CNCCC2=CNC3=C2C=CC(=C3)F.Cl
Standard InChIKey KXOQNPANAFXKTN-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H19F5N2O.ClH/c21-15-4-5-17-14(11-27-18(17)9-15)6-7-26-10-13-2-1-3-16(8-13)28-12-20(24,25)19(22)23;/h1-5,8-9,11,19,26-27H,6-7,10,12H2;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Lu AE58054 Hydrochloride

DescriptionLu AE58054 hydrochloride is an in-vitro potency and selectivity, in-vivo binding affinity and effect of the 5-HT(6)R antagonist with a Ki value of 0.83 nM. IC50 Value: 0.83 nm [1] Target: 5-HT(6)R in vitro: Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. In a 5-HT(6) GTPgammaS efficacy assay Lu AE58054 showed no agonist activity, but demonstrated potent inhibition of 5-HT-mediated activation. Besides medium affinity to adrenergic alpha(1A)- and alpha(1B)-adrenoreceptors, Lu AE58054 demonstrated >50-fold selectivity for more than 70 targets examined [1]. in vivo: Orally administered Lu AE58054 potently inhibited striatal in-vivo binding of the 5-HT(6) antagonist radioligand [(3)H]Lu AE60157, with an ED(50) of 2.7 mg/kg. Steady-state modelling of an acute pharmacokinetic/5-HT(6)R occupancy time-course experiment indicated a plasma EC(50) value of 20 ng/ml. Administration of Lu AE58054 in a dose range (5-20 mg/kg p.o.) leading to above 65% striatal 5-HT(6)R binding occupancy in vivo, reversed cognitive impairment in a rat novel object recognition task induced after subchronic treatment for 7 d with phencyclidine (PCP 2 mg/kg b.i.d., i.p. for 7 d, followed by 7 d drug free). The results indicate that Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia [1]. Clinical trial: Lu-AE58054 Added to Donepezil for the Treatment for Moderate Alzheimer's Disease. Phage2

References:
[1]. Arnt J, et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33. [2]. Witten L, et al. Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine6 (5-HT6) receptors in vivo.

Lu AE58054 Hydrochloride Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Lu AE58054 Hydrochloride Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Lu AE58054 Hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2997 mL 11.4987 mL 22.9975 mL 45.995 mL 57.4937 mL
5 mM 0.4599 mL 2.2997 mL 4.5995 mL 9.199 mL 11.4987 mL
10 mM 0.23 mL 1.1499 mL 2.2997 mL 4.5995 mL 5.7494 mL
50 mM 0.046 mL 0.23 mL 0.4599 mL 0.9199 mL 1.1499 mL
100 mM 0.023 mL 0.115 mL 0.23 mL 0.4599 mL 0.5749 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on Lu AE58054 Hydrochloride

Lu AE58054 hydrochloride is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist with Ki value of 0.83 nM [1].
The serotonin6 receptor (5-HT6R) is one of 14 known 5-HTRs in the serotonin receptor family [1]. It plays an important role in cognitive impairments associated with Alzheimer's disease and schizophrenia [2].
In the 5-HT(6) GTP gamma S efficacy assay, Lu AE58054 showed potent inhibition of 5-HT-mediated activation. Apart from medium affinity to adrenergic alpha (1B)- and alpha(1A)-adrenoreceptors, Lu AE58054 shows >50-fold selectivity compared with more than 70 targets examined [1].
In rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 with ED50 of 2.7 mg/kg. Administration of Lu AE58054 in a dose range (5–20 mg/kg) leading to above 65% 5-HT6R binding, which reversed cognitive impairment in rats treatment with phencyclidine. These results indicate that Lu AE58054 is a potent antagonist of 5-HT6Rs with good oral bioavailability in the rat model of cognitive impairment in schizophrenia [1].
References:
[1]. Arnt J, Bang-Andersen B, Grayson B, et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol, 2010, 13(8): 1021-1033.
[2]. Witten L, Bang-Andersen B, Nielsen SM, et al. Molecular and Cellular Pharmacology
Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine6 (5-HT6) receptors in vivo. Eur J Pharmacol, 2012, 676(1-3): 6-11.

Featured Products
New Products
 

Description

Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a potent and selective 5-HT6 receptor antagonist with a Ki of 0.83 nM.

Keywords:

Lu AE58054 Hydrochloride,467458-02-2,Idalopirdine Hydrochloride,Natural Products,5-HT Receptor, buy Lu AE58054 Hydrochloride , Lu AE58054 Hydrochloride supplier , purchase Lu AE58054 Hydrochloride , Lu AE58054 Hydrochloride cost , Lu AE58054 Hydrochloride manufacturer , order Lu AE58054 Hydrochloride , high purity Lu AE58054 Hydrochloride

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: