BAY-1797

2055602-83-8

416.88

DMSO : 250 mg/mL (599.69 mM; Need ultrasonic)

Membrane Transporter/Ion Channel

BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC₅₀ of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects^[1]. IC50 & Target: IC50: 211 nM (human P2X4), >50 uM (human P2X1), >30 uM (human P2X23), 8.3 uM (human P2X3), 10.6 uM (human P2X7)^[1] In Vitro: BAY-1797 inhibits human, mouse, and rat P2X4 in 1321N1 cells with IC₅₀s of 108 nM, 112 nM, and 233 nM, respectively^[1].
BAY-1797 exerts no measurable activity on hERG and carbonic anhydrase II (both IC₅₀>10 uM). BAY-1797 is also tested against a panel of off-targets, including G-protein coupled receptors (GPCRs), ion channels, kinases, and transporters at 10 uM. An inhibitory activity against the dopamine transporter (DAT, IC₅₀ 2.17 uM) was revealed as the only hit^[1]. 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^[1].
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^[1].
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^[1].