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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $41 | In Stock | In Stock | |
| 5 mg | $83 | In Stock | In Stock | |
| 10 mg | $119 | In Stock | In Stock | |
| 25 mg | $208 | In Stock | In Stock | |
| 50 mg | $312 | In Stock | In Stock | |
| 100 mg | $441 | In Stock | In Stock | |
| 200 mg | $593 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $89 | In Stock | In Stock |
| 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]. |
| Synonyms | Lu AE58054 Hydrochloride, Idalopirdine HCl |
| Molecular Weight | 434.83 |
| Formula | C20H20ClF5N2O |
| Cas No. | 467458-02-2 |
| Smiles | Cl.FC(F)C(F)(F)COc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 50 mg/mL (114.99 mM), Sonication is recommended. DMSO: 20 mg/mL (45.99 mM), Sonication is recommended. H2O: 3 mg/mL (6.9 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.6 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
H2O/DMSO/Ethanol
DMSO/Ethanol
Ethanol
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