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).

For research use only. We do not sell to patients.

A2AR-antagonist-1

A2AR-antagonist-1 Chemical Structure

CAS No. : 2922920-71-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2147 mL 11.0737 mL 22.1474 mL
5 mM 0.4429 mL 2.2147 mL 4.4295 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2147 mL 11.0737 mL 22.1474 mL 55.3685 mL
5 mM 0.4429 mL 2.2147 mL 4.4295 mL 11.0737 mL
10 mM 0.2215 mL 1.1074 mL 2.2147 mL 5.5369 mL
15 mM 0.1476 mL 0.7382 mL 1.4765 mL 3.6912 mL
20 mM 0.1107 mL 0.5537 mL 1.1074 mL 2.7684 mL
25 mM 0.0886 mL 0.4429 mL 0.8859 mL 2.2147 mL
30 mM 0.0738 mL 0.3691 mL 0.7382 mL 1.8456 mL
40 mM 0.0554 mL 0.2768 mL 0.5537 mL 1.3842 mL
50 mM 0.0443 mL 0.2215 mL 0.4429 mL 1.1074 mL
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A2AR-antagonist-1 Related Classifications

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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