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BAY-1797

CAS No. : 2055602-83-8

MCE 站：BAY-1797

产品活性：BAY-1797 是一种高效、具有口服活性的，选择性的 P2X4 拮抗剂，对人 P2X4 的 IC₅₀ 为 211 nM。BAY-1797 在其它 P2X 离子通道上没有或表现出很弱的活性。BAY-1797 具有抗伤害和抗炎作用。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

In Vitro: BAY-1797 inhibits human, mouse, and rat P2X4 in 1321N1 cells with IC₅₀s of 108 nM, 112 nM, and 233 nM, respectively.
BAY-1797 exerts no measurable activity on hERG and carbonic anhydrase II (both IC₅₀>10 μM). BAY-1797 is also tested against a panel of off-targets, including G-protein coupled receptors (GPCRs), ion channels, kinases, and transporters at 10 μM. An inhibitory activity against the dopamine transporter (DAT, IC₅₀ 2.17 μM) was revealed as the only hit.

In Vivo: BAY-1797 (12.5-50 mg/kg; p.o.) shows a significant induction of PGE2 levels in the inflamed paw in the mouse Complete Freund’s Adjuvant (CFA) inflammatory pain model.
BAY-1797 (50 mg/kg; once daily for multiple p.o. administrations) induces a significant reduction of the ipsilateral paw load 24 and 48 h after CFA injection.
BAY-1797 treatment shows the AUC_norm, V_ss and t_1/2 are 1.06 kg h/L, 3.67 L/kg and 2.64 hours, respectively.

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