A2A receptor antagonist 4
A2A receptor antagonist 4 is an orally active A2A adenosine receptor antagonist with an IC50 of 0.8-1.8 nM and a long receptor residence time. A2A receptor antagonist 4 also exhibits antagonistic activity against A1 and A2B receptors, with IC50 values of 140 nM and 12.3-56.9 nM, respectively. A2A receptor antagonist 4 blocks A2A receptor-mediated adenosine signaling and A2B receptor-mediated adenosine signaling, and remains active under adenosine-rich conditions. A2A receptor antagonist 4 dose-dependently reduces metastatic burden in a lung metastasis model. A2A receptor antagonist 4 can be used for research related to fibrosarcoma and lung metastasis.
For research use only. We do not sell to patients.
- CAS No.: 2446776-65-2
- Formula: C25H22FN7O
- Molecular Weight:455.49
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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
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- Purity & Documentation
- References
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Help & FAQs
All Adenosine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
rA2A 1.8 nM (IC50, Low adenosine) |
rA2A 0.8 nM (IC50, High adenosine) |
hA2B 12.3 nM (IC50, Low adenosine) |
hA2B 56.9 nM (IC50, High adenosine) |
A1 140 nM (IC50) |
In Vitro
A2A receptor antagonist 4 exhibits an IC50 of 12.3 nM (low adenosine) and 56.9 nM (100 µM adenosine) for the A2B receptor in HEK293 cAMPZen A2B cells, maintaining nanomolar activity under tumor microenvironment-like high adenosine conditions[1].
A2A receptor antagonist 4 exhibits an IC50 of 140 nM for the A1 receptor in Ba/F3 cells, indicating significantly lower selectivity for A1 over A2A/A2B[1].
A2A receptor antagonist 4 exhibits a receptor residence time of approximately 250 min in a radioligand dissociation assay for the human A2A receptor using [3H]ZM241385, and is a long-acting/slow-dissociating dual A2A/A2B antagonist[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-t | Cmax | CL | Vss | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 0.864 h | 2191 ng·h/mL | 3273 ng/mL | 0.456 L/h/kg | 0.374 L/kg | / |
| Rat[1] | 1 mg/kg | i.v. | 3.39 h | 2537 ng·h/mL | 3007 ng/mL | 0.415 L/h/kg | 1.09 L/kg | / |
| Dog[1] | 1 mg/kg | i.v. | 1.13 h | 1068 ng·h/mL | 1611 ng/mL | 0.47 L/h/kg | 0.53 L/kg | / |
| Monkey[1] | 0.5 mg/kg | i.v. | 0.71 h | 187 ng·h/mL | 403 ng/mL | 2.65 L/h/kg | 1.71 L/kg | / |
| Mice[1] | 3 mg/kg | p.o. | 1.19 h | 4399 ng·h/mL | 3023 ng/mL | / | / | 68 % |
| Rat[1] | 3 mg/kg | p.o. | 3.31 h | 5191 ng·h/mL | 600 ng/mL | / | / | 69 % |
| Dog[1] | 3 mg/kg | p.o. | 1.01 h | 2620 ng·h/mL | 1233 ng/mL | / | / | 41 % |
| Monkey[1] | 3 mg/kg | p.o. | 0.89 h | 2136 ng·h/mL | 637 ng/mL | / | / | 191 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female wild-type C57BL/6 mice were intravenously injected with 1 × 105 MCA205 fibrosarcoma cells to establish a MCA205 fibrosarcoma lung metastasis model[1]
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Dosage:1.5, 5 and 15 mg/kg
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Administration:Oral gavage; twice daily; 15 days
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Result:Significantly and dose-dependently reduced metastatic burden in the aggressive MCA205 pulmonary metastasis model.
Chemical Information
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CAS No. 2446776-65-2
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Molecular Weight 455.49
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Formula C25H22FN7O
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SMILES
O=C(C1=CN2C(C(N)=NC(C3=CC=C(F)C=C3)=C2C4=CN5C(C=C4)=NC=C5C)=N1)NCC6CC6
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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)
A2A receptor antagonist 4 Related Classifications
HY-189446 Related Classifications
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