1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. BAY-1797

BAY-1797 

Cat. No.: HY-130605
Handling Instructions

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.

For research use only. We do not sell to patients.

BAY-1797 Chemical Structure

BAY-1797 Chemical Structure

CAS No. : 2055602-83-8

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Description

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[1].

IC50 & Target

IC50: 211 nM (human P2X4), >50 μM (human P2X1), >30 μM (human P2X23), 8.3 μM (human P2X3), 10.6 μM (human P2X7)[1]

In Vitro

BAY-1797 inhibits human, mouse, and rat P2X4 in 1321N1 cells with IC50s of 108 nM, 112 nM, and 233 nM, respectively[1].
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[1].

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[1].
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[1].
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[1].

Animal Model: Female adult C57BL/6N mice (CFA inflammatory pain model)[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: p.o.; once
Result: Dose-dependently reduced PGE2 concentration in inflamed paw.
Animal Model: Rat male Wistar[1]
Dosage: 1 mg/kg
Administration: i.v. (Pharmacokinetic Analysis)
Result: The AUCnorm, Vss and t1/2 were 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

SMILES

O=C(NC1=CC=C(OC2=CC=CC(Cl)=C2)C(S(=O)(N)=O)=C1)CC3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BAY-1797BAY1797BAY 1797P2X ReceptorP2XRsselectiveP2Xionchannelanti-nociceptiveanti-inflammatoryCompleteFreund’sAdjuvantCFAinflamedpawInhibitorinhibitorinhibit

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