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Adenosine receptor antagonist 2

Cat. No. M40652
Adenosine receptor antagonist 2 Structure
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Biological Activity

Adenosine receptor antagonist 2 is a potent, orally active and antitumor active adenosine receptor A2a/A2b antagonist with IC50 values of 1 nM and 3 nM, respectively.

Chemical Information
Molecular Weight 444.46
Formula C23H21FN8O
CAS Number 2703054-47-9
Form Solid
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Emerson A Lim et al. Clin Cancer Res. Phase Ia/b, Open-Label, Multicenter Study of AZD4635 (an Adenosine A2A Receptor Antagonist) as Monotherapy or Combined with Durvalumab, in Patients with Solid Tumors

[2] Mieko Tokano et al. Immunol Med. Istradefylline, an adenosine A2a receptor antagonist, inhibits the CD4+ T-cell hypersecretion of IL-17A and IL-8 in humans

[3] Amirhossein Bahreyni et al. J Pharm Pharmacol. Therapeutic potency of pharmacological adenosine receptor agonist/antagonist in angiogenesis, current status and perspectives

[4] Sara Redenti et al. Curr Top Med Chem. Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines and Structurally Simplified Analogs. Chemistry and SAR Profile as Adenosine Receptor Antagonists

[5] T M Palmer et al. Mol Pharmacol. 125I-4-(2-[7-amino-2-[2-furyl][1,2,4]triazolo[2,3-a][1,3,5] triazin-5-yl-amino]ethyl)phenol, a high affinity antagonist radioligand selective for the A2a adenosine receptor

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