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GTS-21 99% high purity
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GTS-21
99% Purity GTS-21 CAS 156223-05-1
GTS-21
CAS No. 156223-05-1
Other Names Nefiracetam
MF: C19H22Cl2N2O2
Grade Pharmaceutical Grade
Shelf Life 2 Years
Transport Package Paper Bag or Drum
Specification
1kg/bag; 25kg/drum
Origin China
HS Code 2942000000
Production Capacity 50kg/Year
GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective
alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and
cognition enhancement activity in human clinical trials. Athenagen licensed the exclusive
rights to the compound and a related library of analogs as part of the acquisition of Osprey
Pharmaceutical Company in April 2006. GTS-21 has been studied in multiple Phase I studies
in healthy volunteers and one Phase I/II study in schizophrenic patients. In all studies, the
compound was well tolerated. In a Phase I multi-dose, double-blind, placebo controlled study
in healthy adults, GTS-21 also demonstrated cognitive enhancement across all doses, with a
statistically significant improvement in attention related and memory related tasks.
GTS-21 was O-demethylated to yield compounds that were then subject to glucuronidation.
Three of the metabolites in rat urine were isolated and characterized as 4-OH-GTS-21,
4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. The major urinary metabolites
were 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. In vitro chemical inhibition
of cytochrome P450 in human liver microsomes indicated that CYPIA2 and CYP2E1 were the
isoforms primarily responsible for the O-demethylation of GTS-21, with some contribution from
CYP3A.
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