BX 430 is a selective P2X4 allosteric antagonist (IC50 = 0.54 μM). Exhibits >10-fold selectivity for human P2X4 receptors over P2X1, P2X2, P2X3, P2X5 and P2X7 receptors. Binds noncompetitively at extracellular allosteric site. Effective at human and zebrafish, but not mouse and rat P2X4 receptors.
| Molecular Weight | 413.11 |
| Formula | C15H15Br2N3O |
| CAS Number | 688309-70-8 |
| Solubility (25°C) | DMSO 41.31 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 |
|---|
| UDP-Galactose disodium
UDP-Galactose disodium is a monosaccharide and a P2Y14 receptor agonist with an EC50 value of 0.67 μM. |
| 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. |
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