FR194921 is a blood-brain barrier-permeable A1R adenosine receptor antagonist. The measured Ki values of FR194921 for the human adenosine A1 receptors have been in the low nM range with no binding affinity for A2A and A3 receptors up to 1μM. It is orally active and has good bioavailability. FR194921 was used in a recent study to restore auditory cortex plasticity. Paired with sound exposure, FR194921 resulted in cortical map plasticity and improved auditory perception in adult mice.
| Molecular Weight | 385.46 |
| Formula | C23H23N5O |
| CAS Number | 202646-80-8 |
| Solubility (25°C) | DMSO: 2 mg/mL (warmed) |
| 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 |
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LUF5519 is a ribose-containing adenosine A1 receptor agonist. |
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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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