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BAY-1797

BAY-1797
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Purity:98.74%
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BAY-1797

Catalog No. T10466Cas No. 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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Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
5 mg$80In Stock
10 mg$147In Stock
25 mg$297In Stock
50 mg$555In Stock
100 mg$783In Stock
1 mL x 10 mM (in DMSO)$89In Stock
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Product Introduction

Bioactivity
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.) 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.
Chemical Properties
Molecular Weight416.88
FormulaC20H17ClN2O4S
Cas No.2055602-83-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 250 mg/mL (599.69 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3988 mL11.9939 mL23.9877 mL119.9386 mL
5 mM0.4798 mL2.3988 mL4.7975 mL23.9877 mL
10 mM0.2399 mL1.1994 mL2.3988 mL11.9939 mL
20 mM0.1199 mL0.5997 mL1.1994 mL5.9969 mL
50 mM0.0480 mL0.2399 mL0.4798 mL2.3988 mL
100 mM0.0240 mL0.1199 mL0.2399 mL1.1994 mL

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