TC-G 1004
Names
Biological Activity
[Description]:
TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for hA2A and hA1, respectively[1].
[Related Catalog]:
[Target]
Ki: 0.44 nM (hA2A), 80 nM (hA1)[1].
[In Vitro]
TC-G 1004 (compound 16j) is a highly potent A2A antagonist at both the human and rat receptors with greater than 100× selectivity over hA1[1].
[In Vivo]
TC-G 1004 (compound 16j, 3 mg/kg) displays good in vivo oral activity in rat models for Parkinson’s disease and were advanced to preclinical development[1]. TC-G 1004 (compound 16j) dose-dependently potentiates L-dopa induced rotations with an MED of 3 mg/kg when dosed orally[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C22H27N7O2
[ Molecular Weight ]:
421.49500
[ Exact Mass ]:
421.22300
[ PSA ]:
101.55000
[ LogP ]:
3.62920