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Cat. No.: HY-174413

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A2AAR antagonist 3

A2AAR antagonist 3 is a selective and potent A_2A adenosine receptor (A_2A AR) antagonist with an IC₅₀ of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A_2A AR. A2AAR antagonist 3 demonstrates favorable stability in rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.

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

Formula: C₁₈H₂₀N₈O
Molecular Weight:364.40

Storage:

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

Data Sheet (271 KB)

A2AAR antagonist 3 Chemical Structure

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Fluorescent Dye

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Adenosine Receptor Isoforms :

In Vitro

A2AAR antagonist 3 (Compound 12a) (1 μM, 48 h) restores NECA-suppressed (1 μM, pretreating for 30 min) IL-2 secretion in human peripheral blood mononuclear cells (PBMCs)^[1].

A2AAR antagonist 3 (3.125-100 μM, 24 h) exhibits no significant toxicity towards L929, H9C2, and HTX2426 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

L929 (mouse fibroblasts), H9C2 (rat cardiomyocytes), and HTX2426 (human podocytes).
Concentration:

3.125, 6.25, 12.5, 25, 50, and 100 μM
Incubation Time:

24 h
Result:

Exhibited no significant cytotoxicity towards the L929 cells.
Promoted the proliferation of H9C2 cells at concentrations ranging from 3.125 to 25 μM, and showed a slight inhibitory effect at 50 to 100 μM (cell viability 0f 95 %).
Increased cell viability in HTX2426 cells.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	F
Rat^[1]	20 mg/kg	p.o.	4.56 h	0.25 h	2628.17 μg/L	278170 μg·h/mL	283330 μg·h/mL	58.96 %
Rat^[1]	7 mg/kg	i.v.	3.61 h	0.008 h	5078.88 μg/L	471760 μg·h/mL	3335640 μg·h/mL	/

Chemical Information

Molecular Weight 364.40
Formula C₁₈H₂₀N₈O
SMILES

OC(C)(C)C1=CC=CC(CN2N=NC(C3=NC(N)=NC4=C3C=CN4C)=C2)=N1
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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]. Li Z, et al. Design, synthesis, and biological evaluation of A2A adenosine receptor antagonists containing pyrrolo[2,3-d]pyrimidin-2-amine skeleton. Bioorg Chem. 2025 Jun 3;163:108664. [Content Brief]

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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.

Keywords

100 mg

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Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

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A2AAR antagonist 3

All Adenosine Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

A2AAR antagonist 3 Related Classifications

HY-174413 Related Classifications