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。

BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC 50 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.

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IC50: 211 nM (human P2X4), >50 μM (human P2X1), >30 μM (human P2X23), 8.3 μM (human P2X3), 10.6 μM (human P2X7)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Werner S, et al. Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile. J Med Chem. 2019 Dec 26;62

In Vitro: DMSO : 250 mg/mL (599.69 mM; Need ultrasonic)配制储备液