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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
5 mg | $80 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $555 | In Stock | |
100 mg | $783 | In Stock | |
1 mL x 10 mM (in DMSO) | $89 | In Stock |
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. |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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