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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B607938-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $22.90 | |
B607938-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,334.90 | |
B607938-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $144.90 | |
B607938-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,001.90 | |
B607938-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $459.90 | |
B607938-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $739.90 |
Specifications & Purity | Moligand™, ≥98% |
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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. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-[4-(3-chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide |
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INCHI | InChI=1S/C20H17ClN2O4S/c21-15-7-4-8-17(12-15)27-18-10-9-16(13-19(18)28(22,25)26)23-20(24)11-14-5-2-1-3-6-14/h1-10,12-13H,11H2,(H,23,24)(H2,22,25,26) |
InChi Key | CSJYMAFXYMYNCK-UHFFFAOYSA-N |
Canonical SMILES | C1=CC=C(C=C1)CC(=O)NC2=CC(=C(C=C2)OC3=CC(=CC=C3)Cl)S(=O)(=O)N |
Isomeric SMILES | C1=CC=C(C=C1)CC(=O)NC2=CC(=C(C=C2)OC3=CC(=CC=C3)Cl)S(=O)(=O)N |
PubChem CID | 124125214 |
Molecular Weight | 416.88 |
PubChem CID | 124125214 |
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ChEMBL Ligand | CHEMBL4521594 |
BindingDB Ligand | 50506158 |
CAS Registry No. | 2055602-83-8 |
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Solubility | DMSO: 250 mg/mL (599.69 mM), Sonication is recommended |
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1. Werner S, Mesch S, Hillig RC, Ter Laak A, Klint J, Neagoe I, Laux-Biehlmann A, Dahllöf H, Bräuer N, Puetter V et al.. (2019) 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, 62 (24): (11194-11217). [PMID:31746599] [10.1021/op500134e] |