1. GPCR/G Protein
  2. Adenosine Receptor
  3. A2A receptor antagonist 3

A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively.

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A2A receptor antagonist 3

A2A receptor antagonist 3 Chemical Structure

CAS No. : 2738606-83-0

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Description

A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively[1].

IC50 & Target[1]

A2AR

0.4 nM (Ki)

A2BR

37 nM (Ki)

A1R

107 nM (Ki)

A3R

1467 nM (Ki)

In Vitro

A2A receptor antagonist 3 (Example 92) (24 h) inhibits CD3/CD28 stimulated IL-2 release with an IC50 of 0.004 μM[1].
A2A receptor antagonist 3 (20 min) inhibits pCREB in CD8+T cells in human whole blood with an IC50 of 0.02 μM[1].

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

Molecular Weight

454.52

Formula

C26H26N6O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(O)[C@H](C)NC(C1=NC2=C(C3=CC(C)=NC(C)=C3)C(C4=CC(C#N)=CC=C4)=NN2C=C1)=O

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 (55.00 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 2.2001 mL 11.0006 mL 22.0012 mL
5 mM 0.4400 mL 2.2001 mL 4.4002 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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 2.2001 mL 11.0006 mL 22.0012 mL 55.0031 mL
5 mM 0.4400 mL 2.2001 mL 4.4002 mL 11.0006 mL
10 mM 0.2200 mL 1.1001 mL 2.2001 mL 5.5003 mL
15 mM 0.1467 mL 0.7334 mL 1.4667 mL 3.6669 mL
20 mM 0.1100 mL 0.5500 mL 1.1001 mL 2.7502 mL
25 mM 0.0880 mL 0.4400 mL 0.8800 mL 2.2001 mL
30 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.8334 mL
40 mM 0.0550 mL 0.2750 mL 0.5500 mL 1.3751 mL
50 mM 0.0440 mL 0.2200 mL 0.4400 mL 1.1001 mL
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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.

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Product Name:
A2A receptor antagonist 3
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HY-148076
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