1337962-47-6
Chemical Structure
Taminadenant
Synonym(s): NIR178; PBF509
- CAS No.: 1337962-47-6
- Formula:C10H8BrN7
- Molecular Weight:306.12
IUPAC Name: 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine
InChIKey: ATFXVNUWQOXRRU-UHFFFAOYSA-N
SMILES: BrC(C(N1C=CC=N1)=NC(N2C=CC=N2)=N3)=C3N
Biological Activity: Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response[1][2].
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Taminadenant | 99.84% | Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response. | ||||||||||||||||||||
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Taminadenant (Standard) | ≥98% | Taminadenant (Standard) is the analytical standard of Taminadenant (HY-109139). This product is intended for research and analytical applications. Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparKinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
