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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.

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Formule: C₁₈H₂₀N₈O
Masse moléculaire:364.40

Stockage:

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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Quantité

Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- In Vitro
- Parmacokinetics
Chemical Information
Protocole (1)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform Adenosine Receptor :

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. Further protocols information, click here.

Cell Cytotoxicity Assay^[1]

View Protocol

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

Masse moléculaire 364.40
Formule C₁₈H₂₀N₈O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Protocole

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.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

Calculateur de molarité

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Calculateur de dilution

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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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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