Identification | Back Directory | [Name]
1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- | [CAS]
1038988-11-2 | [Synonyms]
5HT6-ligand-1 5HT6 ligand 1,5HT-6-ligand-1,5HT6ligand1 1-(2-bromobenzenesulfonyl)-4-(4-methylpiperazin-1-ylmethyl)-1H-indole 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- | [Molecular Formula]
C20H22BrN3O2S | [MDL Number]
MFCD31544379 | [MOL File]
1038988-11-2.mol | [Molecular Weight]
448.38 |
Chemical Properties | Back Directory | [Boiling point ]
587.1±60.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
7.57±0.10(Predicted) |
Hazard Information | Back Directory | [Uses]
5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM. | [in vivo]
5HT6-ligand-1 is extensively metabolized in rat liver microsomes whereas in human liver microsomes, 5HT6-ligand-1 is extensively metabolized (90%). The IC50 values for 5HT6-ligand-1 at CYP 3A4 is 35.97%, whereas the IC50 values at CYP 2D6 enzymes is less than 20 μM. 5HT6-ligand-1 at an oral dose of 10 mg/kg is rapidly absorbed in rats with a good oral half-life of 3.17±0.49 h with an oral bioavailability of 29±5%. The observed oral Cmax is 60±44 ng/mL and occurs at 1.83 h. 5HT6-ligand-1 displays an oral exposure of 217±92 ng h/mL. It has a clearance of 220±92 mL/min/kg with a volume of distribution of 32.6±10.7 L/kg for iv dose. Extensive rat metabolism coupled with high clearance could be the possible reason for moderate oral bioavailability showed by 5HT6-ligand-1. Oral administration of 5HT6-ligand-1 reverses the time delay induced memory deficit and statistically significant effect is observed at a dose of 10 mg/kg indicating cognitive improvement potential of the compound 6a[1]. | [IC 50]
5-HT6 Receptor: 1.43 nM (Ki) | [References]
[1] Nirogi RVS, et al. Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands. Bioorg Med Chem Lett 22 (2012) 7431–7435 |
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