8-Aminoadenine is a adenine receptor agonist (Ki = 0.0341 μM in HEK293 cells expressing an adenine binding site). Displays 190-fold increased potency at the human binding site over the rat adenine receptor (rAde1R) (Ki = 6.51 μM).
| Molecular Weight | 150.14 |
| Formula | C5H6N6 |
| CAS Number | 28128-33-8 |
| Solubility (25°C) | DMSO 7.51 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.
[2] Anna Avi, et al. Structural properties of g,t-parallel duplexes
[4] Miriam Frieden, et al. Convenient synthesis of 8-amino-2'-deoxyadenosine
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| A3AR agonist 1
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| A3AR agonist 2
A3AR agonist 2 a selective A3AR agonist (Ki: 22.1 nM). |
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Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. |
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