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Taminadenant

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Chemical Structure| 1337962-47-6 同义名 : NIR178;PBF509
CAS号 : 1337962-47-6
货号 : A232307
分子式 : C10H8BrN7
纯度 : 97%
分子量 : 306.121
MDL号 : MFCD30489281
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 120 mg/mL(392 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Taminadenant is a potent, orally active A2AR antagonist.Taminadenant antagonises A2AR agonist-mediated cAMP accumulation and impedance responses with Kb values of 72.8 nM and 8.2 nM, respectively.Taminadenant reverses dyskinesia in several rat models of dyskinesia, including catalepsy, tremor, and hemiparkinsonism. Parkinson's disease. Taminadenant also inhibits tumour growth when combined with Spartalizumab.Taminadenant reactivates anti-tumour immune responses[1][2].Taminadenant did not show any agonist efficacy in HEK cells permanently expressing human A2ARSNAP, but it completely antagonised agonist-mediated cAMP accumulation with an IC50 of 72.8 ± 17.4 nM in HEK cells expressing A2ARSNAP[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.27mL

0.65mL

0.33mL

16.33mL

3.27mL

1.63mL

32.67mL

6.53mL

3.27mL

参考文献

[1]Núñez F, et al. PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders. Front Pharmacol. 2018 Oct 19;9:1200.

[2]Chiappori AA, et al. Phase I Study of Taminadenant (PBF509/NIR178), an Adenosine 2A Receptor Antagonist, with or without Spartalizumab (PDR001), in Patients with Advanced Non-Small Cell Lung Cancer. Clin Cancer Res. 2022 Jun 1;28(11):2313-2320.