Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases.
MedKoo Cat#: 556046
Name: Lu AF27139
CAS#: 2097117-06-9
Chemical Formula: C21H19ClF3N5O2S
Exact Mass: 497.0900
Molecular Weight: 497.92
Elemental Analysis: C, 50.66; H, 3.85; Cl, 7.12; F, 11.45; N, 14.07; O, 6.43; S, 6.44
The following data is based on the product molecular weight 497.92 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
2914.jpg "Carmustine (98%)")