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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 | Availability | Quantity |
---|---|---|---|
1 mg | 55 € | In Stock | |
2 mg | 75 € | In Stock | |
5 mg | 112 € | In Stock | |
10 mg | 161 € | In Stock | |
25 mg | 282 € | In Stock | |
50 mg | 423 € | In Stock | |
100 mg | 598 € | In Stock | |
200 mg | 805 € | In Stock | |
1 mL x 10 mM (in DMSO) | 120 € | 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]. |
Alias | 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 |
Storage | Powder: -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
DMSO/Ethanol
Ethanol
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