1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Lu AE58054 Hydrochloride (Synonyms: Idalopirdine Hydrochloride)

Cat. No.: HY-14338A Purity: 99.17%
Handling Instructions

Lu 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.

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

Lu AE58054 Hydrochloride Chemical Structure

Lu AE58054 Hydrochloride Chemical Structure

CAS No. : 467458-02-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 290 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 403 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1087 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of Lu AE58054 Hydrochloride:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Lu 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

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (57.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2997 mL 11.4987 mL 22.9975 mL
5 mM 0.4599 mL 2.2997 mL 4.5995 mL
10 mM 0.2300 mL 1.1499 mL 2.2997 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

References
Molecular Weight

434.83

Formula

C₂₀H₂₀ClF₅N₂O

CAS No.

467458-02-2

SMILES

FC1=CC(NC=C2CCNCC3=CC(OCC(F)(F)C(F)F)=CC=C3)=C2C=C1.Cl

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

Room temperature in continental US; may vary elsewhere

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Product Name:
Lu AE58054 Hydrochloride
Cat. No.:
HY-14338A
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Lu AE58054 Hydrochloride

Cat. No.: HY-14338A