country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-144672

Copy Link Print Information

A2A receptor antagonist 2

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A_2A receptor (A_2AR) antagonist with an IC₅₀ of 8.3 nM.

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

CAS No.: 2767206-20-0
Formula: C₂₅H₂₈FN₇O₃
Molecular Weight:493.53

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

A2A receptor antagonist 2 Chemical Structure

CAS No.: 2767206-20-0

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A_2A receptor (A_2AR) antagonist with an IC₅₀ of 8.3 nM^[1].

IC₅₀ & Target

A2AR

8.3 nM (IC₅₀)

All Adenosine Receptor Isoforms :

In Vitro

A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A_2AR agonist) ^[1].
A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

Jurkat T cells
Concentration:

10 μM
Incubation Time:

Overnight
Result:

Increased IL-2 production in the presence of NECA

Cell Cytotoxicity Assay^[1]

View Protocol

Cell Line:

HCT116 and Jurkat T cells
Concentration:

10 μM
Incubation Time:

48 h
Result:

Completely reversed NECA’s suppression of the cytotoxic function of Jurkat T cells.

In Vivo

A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO)^[1].

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

Animal Model:

C57BL/6 mice^[1]
Dosage:

2 or 10 mg/kg
Administration:

Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)

Result:

PK profiles of A2A receptor antagonist 2 (n = 3)^[1]

Parameters
Dosing Route	IV (2 mg/kg)	PO (10 mg/kg)	IP (10mg/kg)
C_max (ng/mL)	1091 ± 129^a	106 ± 33.0	41.8 ± 2.75
AUC_0-last (ng/mL*h)	767 ± 107	145 ± 25.9	812 ± 12.0
AUC_0-t (ng/mL*h)	764 ± 107	139 ± 25.9	444 ± 13.3
T_1/2 (h)	2.05 ± 0.94	2.55 ± 2.39	17.6 ± 0.68
F (%)	/	3.78%	11.6%

^a This value means C₀ = 1091 ± 129 ng/mL

Chemical Information

CAS No. 2767206-20-0
Molecular Weight 493.53
Formula C₂₅H₂₈FN₇O₃
SMILES

NC1=NC(C2=CC=C(O2)C)=C3C(N(C(C=N3)=O)CCN4CCN(C[C@@H]4C)C5=CC=C(C=C5F)OC)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fazhi Yu, et al. Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8H)-one Derivatives as Novel Potent Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2022 Mar 10;65(5):4367-4386. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote