2. GPCR/G Protein
  3. Adenosine Receptor
  4. A2AR-antagonist-1

A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2).

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A2AR-antagonist-1 Chemical Structure

A2AR-antagonist-1 Chemical Structure

CAS No. : 2922920-71-4

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A2AR-antagonist-1 Related Antibodies

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Description

A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2)[1].

IC50 & Target[1]

A2AR

29 nM (IC50)

In Vitro

A2AR-antagonist-1 (0.001-10 μM; 30 min) decreases the level of phosphorylated ERK induced by NECA in HEK293-A2AR cells[1].
A2AR-antagonist-1 (0.1-10 μM; 5 h) inhibits NECA-induced immunological molecules expression and increases effector molecules expression in Jurkat T cells (human immortalized T lymphocyte cell line)[1].
A2AR-antagonist-1 (0.1-10 μM; 48 h) recovers impairment of cytotoxic function of OT-I mouse splenocyte (OT-I CTL) against MC38-OVA cells, enhances T cell’s activation and effector function in vitro[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A2AR-antagonist-1 Related Antibodies

RT-PCR[1]

Cell Line: Jurkat T cells
Concentration: 0.1 μM, 1 μM, and 10 μM
Incubation Time: 5 hours
Result: Reversed NECA (1 μM)-induced up-regulation of immunosuppressive molecules (LAG-3 and TIM-3), and NECA-induced down-regulation of effector molecules (GZMB, IFNG, and IL-2).

Immunofluorescence[1]

Cell Line: Cytotoxic T lymphocytes from OT-I mouse splenocyte (OT-I CTL)
Concentration: 0.1 μM, 1 μM, and 10 μM
Incubation Time: 48 hours
Result: Increased relative killing ability of OT-I CTL according to image.
In Vivo

A2AR-antagonist-1 (100 mg/kg; p.o.; once daily for 23 days) exhibits excellent anti-tumor activity in vivo in C57BL/6 mice bearing colon cancer MC38 cells[1].

Pharmacokinetic Analysis in mouse[1]

Route Dose (mg/kg) Cmax (ng/mL) AUC0-last (ng·h/mL) AUC0-t (ng·h/mL) t1/2 (h) F (%)
i.v. 2 2584 5577 5565 0.93 /
p.o. 10 8823 24008 24003 2.35 86.1

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MC38 xenograft model in mouse[1]
Dosage: 100 mg/kg
Administration: PO; once daily for 23 days
Result: Promoted CD8+ T cell accumulation.
Enhanced antitumor immunity, promoted tumor regression.
Had insignificant effect on body weight of the mice.
Molecular Weight

451.52

Formula

C27H25N5O2
CAS No.
SMILES

O=C(N(CC1=CC=CC(C(O)(C)C)=C1)C=C2)C=C2C3=NC(N)=NC(C4=C(C)C(C#N)=CC=C4)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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A2AR-antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A2AR-antagonist-12922920-71-4Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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