| Bioactivity | ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research[1]. |
| Target | Ki: 12 nM (adenosine A2A receptor), 197 nM (adenosine A1 receptor) |
| Invitro | ST4206 inhibits agonist-induced cAMP accumulation with an IC50 of 990 nM[1]. |
| In Vivo | ST4206 (10, 20, and 40 mg/kg, p.o.) antagonizes haloperidol-induced catalepsy, and increases motor activity in a dose dependent manner in mice.ST4206 (20 and 40 mg/kg) significantly increases the number of contralateral turns induced by l-DOPA in rats[1]. ST4206 is orally active at concentrations of 10, 20, and 40 mg/kg in haloperidol-induced catalepsy in mice[2]. |
| Name | ST4206 |
| CAS | 1246018-36-9 |
| Formula | C12H14N8O |
| Molar Mass | 286.29 |
| 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]. Maria Antonietta Stasi, et al. Animal models of Parkinson׳s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). Eur J Pharmacol. 2015 Aug 15;761 [2]. de Lera Ruiz M, et al. Adenosine A2A receptor as a drug discovery target. J Med Chem. 2014 May 8;57(9):3623-50. |