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.
For research use only. We do not sell to patients.
- CAS No.: 2570904-69-5
- Formula: C21H22N6O2
- Molecular Weight:390.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Adenosine Receptor Isoforms
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Biological Activity
|
A1 1.5 nM (Ki) |
A2A 0.6 nM (Ki) |
A2B 21 nM (Ki) |
MMP-2 |
MMP-8 |
MMP-9 |
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.
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Cell Line:A1R-overexpressing SK-BR-3 cells
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Concentration:10 and 100 nM
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Incubation Time:30 mins
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Result:Reduced the phosphorylation of ERK and JNK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice bearing CT26 tumors[1]
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Dosage:50 mg/kg
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Administration:Orally administration, twice a day for 14 days
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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.
Chemical Information
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CAS No. 2570904-69-5
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Molecular Weight 390.44
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Formula C21H22N6O2
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Adenosine receptor antagonist 7 Related Classifications
HY-179248 Related Classifications
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