ABT-702 dihydrochloride is a potent non-nucleoside adenosine kinase inhibitor, selective over other sites of adenosine interaction like A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase. ABT-702 potently inhibits the activity of rat brain cytosolic AK in a concentration-dependent manner with an IC50 value of 1.7 nM. ABT-702 also potently inhibits AK activity in intact cultured IMR-32 human neuroblastoma cells (IC50=51 nM).
| Molecular Weight | 536.25 |
| Formula | C22H21BrCl2N6O |
| CAS Number | 1188890-28-9 |
| Solubility (25°C) | DMSO 30 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.
| Related Adenosine Deaminase Products |
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Rebecsinib, an RNA adenosine deaminase (ADAR) inhibitor, reverses malignant over-editing by inhibiting ADAR1 p150-driven self-renewal of leukemic stem cells. |
| FR221647
FR221647 is an orally active non-nucleoside inhibitor of adenosine deaminase. |
| Hibifolin
Hibifolin, a flavonol glycoside, is a potential inhibitor of adenosine deaminase (ADA), with a Ki of 49.92 μM. Hibifolin protects neurons against beta-amyloid-induced neurotoxicity. |
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1-Deazaadenosine is a adenosine deaminase inhibitor. |
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