Namodenoson (also known as 2-Cl-IB-MECA and CF-102) is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist (Ki=0.33 nM) with potential antineoplastic activity. Namodenoson selectively binds to and activates the cell surface-expressed A3AR, deregulating Wnt and NF-kB signal transduction pathways downstream, which may result in apoptosis of A3AR-expressing tumor cells. In human ADF cells of astroglial lineage, 100 nM Namodenoson (2-Cl-IB-MECA) caused a marked reorganization of the cytoskeleton, with appearance of stress fibres and numerous cell protrusions.
In vivo, administration of 200 μg/kg Namodenoson (2-Cl-IB-MECA) resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations.
| Molecular Weight | 544.73 |
| Formula | C18H18ClIN6O4 |
| CAS Number | 163042-96-4 |
| Solubility (25°C) | DMSO ≥ 25 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.
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| A3AR agonist 1
A3AR agonist 1 is an A3AR agonist (Ki: 25.8 nM). |
| A3AR agonist 2
A3AR agonist 2 a selective A3AR agonist (Ki: 22.1 nM). |
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