| 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. |