| Name | BAY-1797 |
| 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. |
| 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.) significantly induces PGE2 levels in the inflamed paw in the mouse Complete Freund’s Adjuvant (CFA) inflammatory pain model. At 50 mg/kg daily, BAY-1797 significantly reduces ipsilateral paw load 24 and 48 hours post-CFA injection. Pharmacokinetic parameters include AUCnorm of 1.06 kg h/L, Vss of 3.67 L/kg, and t1/2 of 2.64 hours. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 250 mg/mL (599.69 mM), Sonication is recommended.
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| Keywords | paw | ion | inhibit | anti-inflammatory | BAY-1797 | CFA | Complete | BAY1797 | P2XRs | Freund’s | selective | channel | P2X Receptor | BAY 1797 | inflamed | Inhibitor | Adjuvant | P2X | anti-nociceptive |
| Inhibitors Related | Opiranserin hydrochloride | Aurintricarboxylic acid | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | JNJ-55308942 | JNJ-42253432 | Ivermectin | Lappaconitine | CTP disodium dihydrate | Brilliant blue G-250 |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
