| Identification | Back Directory | [Name]
BAY-1797 | [CAS]
2055602-83-8 | [Synonyms]
BAY-1797
paw,ion,inhibit,anti-inflammatory,CFA,Complete,P2XRs,BAY-1797,Freund’s,selective,channel,P2X Receptor,inflamed,Inhibitor,BAY1797,Adjuvant,BAY 1797,P2X,anti-nociceptive | [Molecular Formula]
C20H17ClN2O4S | [MOL File]
2055602-83-8.mol | [Molecular Weight]
416.88 |
| Chemical Properties | Back Directory | [density ]
1.414±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (>25 mg/ml) | [form ]
solid | [pka]
9.84±0.60(Predicted) | [color ]
Pale brown | [Stability:]
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | [InChIKey]
CSJYMAFXYMYNCK-UHFFFAOYSA-N | [SMILES]
ClC1=CC=CC(OC2=C(C=C(NC(CC3=CC=CC=C3)=O)C=C2)S(=O)(N)=O)=C1 |
| Hazard Information | Back Directory | [Description]
BAY-1797 (2055602-83-8) is a selective P2X4 receptor antagonist (IC50 = 211 nM HEK cellular assay; P2X4 calcium influx based assays – hIC50 = 108 nM, mIC50 = 112 nM, rIC50 = 233 nM).1 Displayed antinociceptive and anti-inflammatory effects in mouse CFA inflammatory pain models. | [Uses]
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]. | [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. |
| [IC 50]
P2X4 Receptor | [storage]
Store at -20°C | [References]
Werner 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 11194 |
|
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
|