Lu AF27139 is a selective antagonist of the P2X7 receptor, exhibiting potent inhibitory activity with IC50 values of 12 nM and 2.4 nM for human and rat receptors, respectively. Additionally, it demonstrates effective inhibition in mouse, human, and rat models with Kis of 22, 54, and 13 nM. Due to its favorable pharmacokinetic profile, including oral activity and CNS penetration, Lu AF27139 is a valuable tool for investigating central nervous system diseases.
Lu AF27139 is a selective antagonist of the P2X7 receptor, exhibiting potent inhibitory activity with IC50 values of 12 nM and 2.4 nM for human and rat receptors, respectively. Additionally, it demonstrates effective inhibition in mouse, human, and rat models with Kis of 22, 54, and 13 nM. Due to its favorable pharmacokinetic profile, including oral activity and CNS penetration, Lu AF27139 is a valuable tool for investigating central nervous system diseases.
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