GW791343 trihydrochloride is a non-competitive human P2X (7) receptor inhibitor with pIC50 of about 7.1. GW791343 trihydrochloride exhibits negative allosteric effects at the human P2X (7) receptor but is a positive allosteric modulator of the rat P2X (7) receptor. GW791343 trihydrochloride competitively interacted at the ATP binding site and so were probably negative allosteric modulators of the P2X (7) receptor. GW791343 trihydrochloride increased responses to BzATP at the F95L mutant receptor, although the magnitude of this effect was not as marked as at the rat ECD, rat–human or domain 1 receptor.
| Molecular Weight | 483.81 |
| Formula | C20H24F2N4O.3HCl |
| CAS Number | 309712-55-8 |
| Solubility (25°C) | DMSO |
| 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.
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Purotoxin 1 is a P2X3 receptor inhibitor. |
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| 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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