1. GPCR/G Protein
  2. Adenosine Receptor
  3. Adenosine receptor antagonist 7

Adenosine receptor antagonist 7 is an orally active triple A1/A2A/A2B adenosine receptor antagonist with Ki values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC50 = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer.

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Adenosine receptor antagonist 7

Adenosine receptor antagonist 7 Chemical Structure

CAS No. : 2570904-69-5

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Description

Adenosine receptor antagonist 7 is an orally active triple A1/A2A/A2B adenosine receptor antagonist with Ki values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC50 = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer[1].

IC50 & Target[1]

A1

1.5 nM (Ki)

A2A

0.6 nM (Ki)

A2B

21 nM (Ki)

In Vitro

Adenosine receptor antagonist 7 (Compound 14a) (0.32-1000 nM, 30 mins) inhibits NECA (HY-103173)-induced cAMP accumulation in human CD8+T cells (IC50 = 18 nM)[1].
Adenosine receptor antagonist 7 (10-100 nM, 30 mins) inhibits the phosphorylation of ERK and JNK, downregulates the mRNA expression of MMP-2 and MMP-9 in A1R-overexpressing SK-BR-3 cells[1].

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

Western Blot Analysis[1]

Cell Line: A1R-overexpressing SK-BR-3 cells
Concentration: 10 and 100 nM
Incubation Time: 30 mins
Result: Reduced the phosphorylation of ERK and JNK.
In Vivo

Adenosine receptor antagonist 7 (Compound 14a) (50 mg/kg, p.o., twice a day for 14 days) inhibits tumor growth in BALB/c nude mice bearing CT26 tumors[1].

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

Animal Model: BALB/c nude mice bearing CT26 tumors[1]
Dosage: 50 mg/kg
Administration: Orally administration, twice a day for 14 days
Result: Inhibited tumor growth without adverse reactions such as weight loss.
Increased the number of tumor-infiltrating effector T cells and improved the CD8+/Treg ratio when combined with Avelumab.
Molecular Weight

390.44

Formula

C21H22N6O2

CAS No.
SMILES

NC1=NC(N2C=CN=C2)=C(C(C3=CC(N4CC[C@H](C4)OC)=CC(OC)=C3)=C1)C#N

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Storage

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

Purity & Documentation
References
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  • 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:
Adenosine receptor antagonist 7
Cat. No.:
HY-179248
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