Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
5 mg | In stock | $ 80.00 | |
10 mg | In stock | $ 147.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 555.00 | |
100 mg | In stock | $ 783.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 89.00 |
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. |
Targets&IC50 | human P2X7:10.6 μM , human P2X4:211 nM , human P2X23:>30 μM , human P2X1:>50 μM , human P2X3:8.3 μM |
In vitro | 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 | 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. |
Molecular Weight | 416.88 |
Formula | C20H17ClN2O4S |
CAS No. | 2055602-83-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (599.69 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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BAY-1797 2055602-83-8 Membrane transporter/Ion channel Neuroscience P2X Receptor paw ion inhibit anti-inflammatory CFA Complete BAY1797 P2XRs Freund’s selective channel BAY 1797 inflamed Inhibitor Adjuvant P2X anti-nociceptive inhibitor