Basic information Safety Supplier Related

1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-

Basic information Safety Supplier Related

1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]- Basic information

Product Name:
1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-
Synonyms:
  • 1H-Indole, 1-[(2-bromophenyl)sulfonyl]-4-[(4-methyl-1-piperazinyl)methyl]-
  • 5HT6-ligand-1
  • 1-(2-bromobenzenesulfonyl)-4-(4-methylpiperazin-1-ylmethyl)-1H-indole
  • 5HT6 ligand 1,5HT-6-ligand-1,5HT6ligand1
CAS:
1038988-11-2
MF:
C20H22BrN3O2S
MW:
448.38
Mol File:
1038988-11-2.mol
More
Less

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)
More
Less

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]-Supplier

BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
cjbscvictory
Tel
13348960310
Email
3003867561@qq.com