BAY-1797

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

Product information

CAS Number: 2055602-83-8

Molecular Weight: 416.88

Formula: C20H17ClN2O4S

Chemical Name: N-[4-(3-chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide

Smiles: NS(=O)(=O)C1=CC(=CC=C1OC1=CC(Cl)=CC=C1)NC(=O)CC1C=CC=CC=1

InChiKey: CSJYMAFXYMYNCK-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (599.69 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BAY-1797 inhibits human, mouse, and rat P2X4 in 1321N1 cells with IC50s of 108 nM, 112 nM, and 233 nM, respectively. BAY-1797 exerts no measurable activity on hERG and carbonic anhydrase II (both IC50>10 μM). BAY-1797 is also tested against a panel of off-targets, including G-protein coupled receptors (GPCRs), ion channels, kinases, and transporters at 10 μM. An inhibitory activity against the dopamine transporter (DAT, 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. administrations) 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.

Products are for research use only. Not for human use.