Catalog No.: PC-35779Not For Human Use, Lab Use Only.
PBF509 (Taminadenant, PBF-509, NIR 178) is a novel selective and potent Adenosine A2A Receptor (A2AR) antagonist, antagonizes A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 and 8.2 nM, respectively.
PBF509 (Taminadenant, PBF-509, NIR 178) is a novel selective and potent Adenosine A2A Receptor (A2AR) antagonist, antagonizes A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 and 8.2 nM, respectively.
PBF509 (orally) antagonized haloperidol-mediated catalepsy, reduced pilocarpine-induced tremulous jaw movements and potentiated the number of contralateral rotations induced by L-3,4-dihydroxyphenylalanine (L-DOPA) in unilaterally 6-OHDA-lesioned rats.
PBF509 (3 mg/kg) inhibited L-DOPA-induced dyskinesia (LID), showing not only its efficacy on reversing parkinsonian motor impairments but also acting as antidyskinetic agent; increased responsiveness of human tumor-infiltrating lymphocytes when combined with anti-PD-1 or anti-PD-L1.
Physicochemical Properties
M.Wt
306.127
Formula
C10H8BrN7
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine
References
1. Núñez F, et al. Front Pharmacol. 2018 Oct 19;9:1200.
2. Mediavilla-Varela M, et al. Neoplasia. 2017 Jul;19(7):530-536.
