P2X4 antagonist-1
Based on 1 Customer Validation
P2X4 antagonist-1 is a P2X4 receptor antagonist with an IC50 of 15 nM. P2X4 antagonist-1 inhibits ATP (HY-B2176)-induced calcium influx. P2X4 antagonist-1 can be used for the research of pain syndromes, endometriosis, cancer.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 2055601-42-6
- Formula: C20H15Cl3N2O4S
- Molecular Weight:485.77
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All P2X Receptor Isoforms
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Biological Activity
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P2X4 Receptor 15 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
15 nM
Compound: 24
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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] |
P2X4 antagonist-1 (Compound 24) inhibits ATP-induced calcium influx in human P2X4-expressing HEK cells with an IC50 of 15 nM[1].
P2X4 antagonist-1 (example 104) potently inhibits human P2X4 receptor with an average IC50 of 15 nM, with average efficacies of 78%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2055601-42-6
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Appearance Solid
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Molecular Weight 485.77
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Formula C20H15Cl3N2O4S
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Color White to off-white
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SMILES
ClC1=CC=CC(OC2=C(S(=O)(N)=O)C=C(NC(CC3=C(Cl)C=CC=C3Cl)=O)C=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (205.86 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (5.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Werner S, et al. 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. 2019 Dec 26;62(24):11194-11217. [Content Brief]
[2]. Werner S, et al. Aromatic sulfonamide derivatives. Germany, WO2016198374 A. 2016-12-15.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0586 mL | 10.2929 mL | 20.5859 mL | 51.4647 mL |
| 5 mM | 0.4117 mL | 2.0586 mL | 4.1172 mL | 10.2929 mL | |
| 10 mM | 0.2059 mL | 1.0293 mL | 2.0586 mL | 5.1465 mL | |
| 15 mM | 0.1372 mL | 0.6862 mL | 1.3724 mL | 3.4310 mL | |
| 20 mM | 0.1029 mL | 0.5146 mL | 1.0293 mL | 2.5732 mL | |
| 25 mM | 0.0823 mL | 0.4117 mL | 0.8234 mL | 2.0586 mL | |
| 30 mM | 0.0686 mL | 0.3431 mL | 0.6862 mL | 1.7155 mL | |
| 40 mM | 0.0515 mL | 0.2573 mL | 0.5146 mL | 1.2866 mL | |
| 50 mM | 0.0412 mL | 0.2059 mL | 0.4117 mL | 1.0293 mL | |
| 60 mM | 0.0343 mL | 0.1715 mL | 0.3431 mL | 0.8577 mL | |
| 80 mM | 0.0257 mL | 0.1287 mL | 0.2573 mL | 0.6433 mL | |
| 100 mM | 0.0206 mL | 0.1029 mL | 0.2059 mL | 0.5146 mL |
P2X4 antagonist-1 Related Classifications
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