PeptideDB

TC-G 1004

CAS: 1061747-72-5 F: C22H27N7O2 W: 421.50

TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for
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Bioactivity 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].
Target Ki: 0.44 nM (hA2A), 80 nM (hA1).
Invitro 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].
Name TC-G 1004
CAS 1061747-72-5
Formula C22H27N7O2
Molar Mass 421.50
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Xiaohu Zhang, et al. Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease. J Med Chem. 2008 Nov 27;51(22):7099-110.