A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
| Molecular Weight | 606.57 |
| Formula | C33H29NNaO9 |
| CAS Number | 475205-49-3 (free base) |
| Solubility (25°C) | Water ≥ 90 mg/mL |
| Storage | 2-8°C, dry, sealed |
| 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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