BAY-1797
Based on 4 publication(s) in Google Scholar
BAY-1797, a chemical probe, 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.76%
- No. CAS: 2055602-83-8
- Fòrmula: C20H17ClN2O4S
- Peso molecular:416.88
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BAY-1797
MoreVer todos los productos específicos de isoformas P2X Receptor
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Actividad biológica
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P2X4 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
211 nM
Compound: 10; BAY-1797
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Antagonist activity at human P2X4 receptor tranfected in HEK293 cells assessed as inhibition of Bz-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay
Antagonist activity at human P2X4 receptor tranfected in HEK293 cells assessed as inhibition of Bz-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay
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[PMID: 31746599] |
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 shows an inhibitory activity against the dopamine transporter (DAT, IC50 2.17 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female adult C57BL/6N mice (CFA inflammatory pain model)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:p.o.; once
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Result:Dose-dependently reduced PGE2 concentration in inflamed paw.
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Animal Model:Rat male Wistar[1]
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Dosage:1 mg/kg
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Administration:i.v. (Pharmacokinetic Analysis)
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Result:The AUCnorm, Vss and t1/2 were 1.06 kg h/L, 3.67 L/kg and 2.64 hours, respectively.
Chemical Information
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No. CAS 2055602-83-8
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Appearance Solid
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Peso molecular 416.88
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Fòrmula C20H17ClN2O4S
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C(OC2=CC=CC(Cl)=C2)C(S(=O)(N)=O)=C1)CC3=CC=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
iScience
M1-like macrophages regulate T cell infiltration in colorectal cancer through P2X4 receptor. [Abstract]2025 Sep 5;28(10):113517. PMID: 41031375 -
FASEB J
Nucleotide receptors mediate protection against neonatal sepsis and meningitis caused by alpha-hemolysin expressing Escherichia coli K1. [Abstract]2022 Mar;36(3):e22197. PMID: 35147989 -
Solvente y solubilidad
DMSO : 250 mg/mL (599.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3988 mL | 11.9939 mL | 23.9877 mL | 59.9693 mL |
| 5 mM | 0.4798 mL | 2.3988 mL | 4.7975 mL | 11.9939 mL | |
| 10 mM | 0.2399 mL | 1.1994 mL | 2.3988 mL | 5.9969 mL | |
| 15 mM | 0.1599 mL | 0.7996 mL | 1.5992 mL | 3.9980 mL | |
| 20 mM | 0.1199 mL | 0.5997 mL | 1.1994 mL | 2.9985 mL | |
| 25 mM | 0.0960 mL | 0.4798 mL | 0.9595 mL | 2.3988 mL | |
| 30 mM | 0.0800 mL | 0.3998 mL | 0.7996 mL | 1.9990 mL | |
| 40 mM | 0.0600 mL | 0.2998 mL | 0.5997 mL | 1.4992 mL | |
| 50 mM | 0.0480 mL | 0.2399 mL | 0.4798 mL | 1.1994 mL | |
| 60 mM | 0.0400 mL | 0.1999 mL | 0.3998 mL | 0.9995 mL | |
| 80 mM | 0.0300 mL | 0.1499 mL | 0.2998 mL | 0.7496 mL | |
| 100 mM | 0.0240 mL | 0.1199 mL | 0.2399 mL | 0.5997 mL |
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