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A2AR-antagonist-1

Catalog No. T72626 CAS 2922920-71-4

A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].

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A2AR-antagonist-1, CAS 2922920-71-4

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].
Targets&IC50	A2AR:29 nM
In vitro	A2AR-antagonist-1 (0.001-10 μM; 30 minutes) reduces NECA-induced phosphorylation of ERK levels in HEK293-A2AR cells [1]. At concentrations of 0.1-10 μM over 5 hours, this compound inhibits NECA-induced expression of immune molecules and increases the expression of effector molecules in Jurkat T cells (human immortalized T lymphocyte line) [1]. Furthermore, A2AR-antagonist-1 (0.1-10 μM; 48 hours) restores the impaired cytotoxic function of OT-I mouse splenocytes (OT-I CTL) against MC38-OVA cells and enhances in vitro T cell activation and effector functions [1].
In vivo	A2AR-antagonist-1 (100 mg/kg; oral administration; once daily for 23 days) demonstrated remarkable antitumor activity in C57BL/6 mice carrying MC38 colon carcinoma cells [1]. Pharmacokinetic analysis in mice [1] revealed the following: Route Dose (mg/kg) C max (ng/mL) AUC 0-last (ng·h/mL) AUC 0-t (ng·h/mL) t 1/2 (h) F (%) for intravenous (i.v.) administration at 2 mg/kg resulted in a C max of 2584 ng/mL, AUC 0-last of 5577 ng·h/mL, AUC 0-t of 5565 ng·h/mL, and a half-life (t 1/2) of 0.93 h, while oral (p.o.) administration at 10 mg/kg achieved a C max of 8823 ng/mL, AUC 0-last of 24008 ng·h/mL, AUC 0-t of 24003 ng·h/mL, t 1/2 of 2.35 h, and bioavailability (F) of 86.1%.

Molecular Weight	451.52
Formula	C27H25N5O2
CAS No.	2922920-71-4

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

A2AR-antagonist-1 2922920-71-4 GPCR/G Protein Neuroscience Adenosine Receptor inhibitor inhibit

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