AF-353 is a novel, potent and orally bioavailable P2X3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). AF-353 administered orally to rats and found to produce highly significant prevention and reversal of bone cancer pain behaviour. AF-353 is an excellent in vivo tool compound for study of these channels in animal models and demonstrates the feasibility of identifying and optimizing molecules into potential clinical candidates, and, ultimately, into a novel class of therapeutics for the treatment of pain-related disorders.
| Molecular Weight | 400.21 |
| Formula | C14H17IN4O2 |
| CAS Number | 865305-30-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 80 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 P2 Receptor Products |
|---|
| Purotoxin 1
Purotoxin 1 is a P2X3 receptor inhibitor. |
| P2X2/3 modulator-1
P2X2/3 modulator-1 is a P2X2/3 modulator. |
| P2X7-IN-2 TFA
P2X7-IN-2 TFA is a P2X7 receptor inhibitor. |
| NP-1815-PX
NP-1815-PX is a potent and selective P2X4R antagonist. |
| P2X3-IN-1
P2X3-IN-1 is an inhibitor of P2X3 receptor. |
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