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Idalopirdine Hydrochloride

Catalog No. T22936Cas No. 467458-02-2
Alias Lu AE58054 Hydrochloride, Idalopirdine HCl

Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).

Idalopirdine Hydrochloride

Idalopirdine Hydrochloride

Purity: 99.97%
Catalog No. T22936Alias Lu AE58054 Hydrochloride, Idalopirdine HClCas No. 467458-02-2
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).
Pack SizePriceAvailabilityQuantity
1 mg$58In Stock
2 mg$79In Stock
5 mg$118In Stock
10 mg$170In Stock
25 mg$297In Stock
50 mg$446In Stock
100 mg$630In Stock
200 mg$848In Stock
1 mL x 10 mM (in DMSO)$127In Stock
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Purity:99.97%
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Product Introduction

Bioactivity
Description
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).
Targets&IC50
5-HT6 receptor:0.83 nM(Ki)
In vitro
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 vivo
In the rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 (ED50: 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].
AliasLu AE58054 Hydrochloride, Idalopirdine HCl
Chemical Properties
Molecular Weight434.83
FormulaC20H20ClF5N2O
Cas No.467458-02-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 50 mg/mL (114.99 mM)
DMSO: 20 mg/mL (45.99 mM)
H2O: 3 mg/mL (6.90 mM, with ultrasonic and warming), Sonication and heating are recommended.
Solution Preparation Table
H2O/DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.2997 mL11.4987 mL22.9975 mL114.9875 mL
5 mM0.4599 mL2.2997 mL4.5995 mL22.9975 mL
DMSO/Ethanol
1mg5mg10mg50mg
10 mM0.2300 mL1.1499 mL2.2997 mL11.4987 mL
20 mM0.1150 mL0.5749 mL1.1499 mL5.7494 mL
Ethanol
1mg5mg10mg50mg
50 mM0.0460 mL0.2300 mL0.4599 mL2.2997 mL
100 mM0.0230 mL0.1150 mL0.2300 mL1.1499 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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