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1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- manufacturers
- 5HT6-ligand-1
-
- $83.00
-
2026-05-11
- CAS:1038988-11-2
- Purity: 99.93%
- Supply Ability: 10g
- 5HT6-ligand-1
-
- $83.00
-
2026-05-11
- CAS:1038988-11-2
- Purity: 99.93%
- Supply Ability: 10g
- 5HT6-ligand-1
-
- $118.00
-
2025-04-27
- CAS:1038988-11-2
- Purity: 98.48%
- Supply Ability: 10g
|
| | 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Basic information |
| | 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Chemical Properties |
| 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) |
| | 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Usage And Synthesis |
| 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 |
| | 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Preparation Products And Raw materials |
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