BAY-1797 , CAS No.2055602-83-8, Antagonist of P2X4

Item Number

B607938

• Specifications & Purity: Moligand™, ≥98%
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: ANTAGONIST
• Mechanism of action: Antagonist of P2X4

Product Description

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

Target activity

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

In vitro activity

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

In vivo activity

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.) induces a significant reduction of the ipsilateral paw load 24 and 48 h after CFA injection. BAY-1797 treatment shows the AUCnorm, Vss, and t1/2 are 1.06 kg h/L, 3.67 L/kg, and 2.64 hours, respectively.