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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-PBF509
PBF509

Chemical Structure : PBF509

CAS No.: 1337962-47-6

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PBF509 (Taminadenant, PBF-509, PBF 509, NIR 178)

货号: 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.

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10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2180 In stock
100 mg ￥3180 In stock
250 mg Get quote
1 g Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 306.127
分子式 C10H8BrN7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine

参考文献

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.

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