LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury.
| Molecular Weight | 414.33 |
| Formula | C22H21Cl2N3O |
| CAS Number | 1116652-18-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 20 mg/mL (ultrasonic and warming and heat to 60°C) |
| Storage | Powder -20°C |
| 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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