Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab. Taminadenant reactivate the antitumor immune response.
| Molecular Weight | 306.12 |
| Formula | C10H8BrN7 |
| CAS Number | 1337962-47-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| 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 Receptor Products |
|---|
| LUF5519
LUF5519 is a ribose-containing adenosine A1 receptor agonist. |
| LUF6258
LUF6258 is a hybrid ortho/allosteric ligand of the adenosine A(1) receptor. |
| 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). |
| Inupadenant hydrochloride
Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. |
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