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BAY-1797

Catalog No. T10466   CAS 2055602-83-8

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.

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BAY-1797 Chemical Structure
BAY-1797, CAS 2055602-83-8
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
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Purity: 98.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (599.69 mM), sonification is recommended.

TargetMolReferences and Literature

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(24):11194-11217.

Related compound libraries

This product is contained In the following compound libraries:
Immunology/Inflammation Compound Library Anti-Aging Compound Library NO PAINS Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Anti-Cancer Compound Library Anti-Fibrosis Compound Library Orally Active Compound Library

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Keywords

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

 

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