Taminadenant free base · Synonyms: NIR178 | PBF509

Taminadenant is a highly potent and orally active adenosine A2A receptor antagonist.

For research use only. Not for human or veterinary use.

Target Adenosine Receptor

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Taminadenant structure

CAS No.: 1337962-47-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 398.00	BP-01018-1g	In stock	Get quote
2 g	USD 650.00	BP-01018-2g	In stock	Get quote
5 g	USD 1,585.00	BP-01018-5g	In stock	Get quote
10 g	Inquire	BP-01018-10g	In stock	Inquire
20 g	Inquire	BP-01018-20g	In stock	Inquire

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Description

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. Taminadenant reactivate the antitumor immune response.

Identifiers

SMILES: BrC(C(N1C=CC=N1)=NC(N2C=CC=N2)=N3)=C3N
InChIKey: ATFXVNUWQOXRRU-UHFFFAOYSA-N

Specifications

MW (average): 306.1210
Formula: C₁₀H₈BrN₇
CAS No.: 1337962-47-6
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 125 mg/mL

Documents

References

[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.

Same target

Search Adenosine Receptor

Same research area

Search Neurological Disease