BAY 60-6583 is a potent adenosine receptor A2b (A2bR) partial agonist (Ki against 0.3 nM [3H]PSB-603 for binding human/mouse/rat A2bR = 114/136/100 nM) that selectively induces cAMP-dependent transcription activity in CHO transfectants expressing human A2bR (EC50 ~100 nM), but not A1R or A2aR, while exhibiting no affinity toward human/rat/mouse A2aR. BAY 60-6583 also displays low-affinity antagonistic activity toward A1R (Ki against 1 nM [3H]CCPA for binding human/mouse/rat A1R = 387/351/514 nM; IC50 = 7.4 μM against 100 nM CCPA-induced hA1R β-arrestin recruitment) and A3R (Ki against 10 nM [3H]NECA for binding human/mouse/rat A3R = 223/3920/2750 nM; IC50 = 6.7 μM against 30 nM Cl-IB-MECA-induced hA3R β-arrestin recruitment). BAY 60-6583 is widely administered in animals in vivo via i.p. (0.1-80 mg/kg) or i.v. (0.2-2 mg/kg) for studying A2bR-mediated biological responses.
| Molecular Weight | 379.44 |
| Formula | C19H17N5O2S |
| CAS Number | 910487-58-0 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[3] Sonja Hinz, et al. Tritium-labeled agonists as tools for studying adenosine A 2B receptors
[4] Sonja Hinz, et al. BAY60-6583 acts as a partial agonist at adenosine A2B receptors
[5] G Ortore, et al. A2B receptor ligands: past, present and future trends
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