Taminadenant_product_DataBase

Bioactivity

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].

Target

Adenosine receptor

Invitro

Taminadenant (PBF509) does not show any agonist efficacy in HEK cells permanently expressing the human A2ARSNAP, but completely antagonizes the agonist-mediated cAMP accumulation in A2ARSNAP expressing HEK cells with an IC50 of 72.8 ± 17.4 nM[1].

In Vivo

Taminadenant (PBF509) (0.3, 3, 7.5, 10, or 30 mg/kg; p.o.; single dosage) attenuates the cataleptic effects of Haloperidol, attenuates pilocarpine-induced tremulous jaw movement, enhances the effects of L-DOPA, shows a robust antiparkinsonian activity and displays antidyskinetic efficacy[1]. Animal Model:

Name

Taminadenant

CAS

1337962-47-6

Formula

C10H8BrN7

Molar Mass

306.12

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Taminadenant

CAS: 1337962-47-6 F: C10H8BrN7 W: 306.12