BX430
Based on 1 Customer Validation
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.21%
- CAS No.: 688309-70-8
- Formule: C15H15Br2N3O
- Masse moléculaire:413.11
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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P2X4 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.54 μM
Compound: BX430
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Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-evoked current by patch clamp assay
Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-evoked current by patch clamp assay
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[PMID: 31532206] |
| HEK293 | IC50 |
1.3 μM
Compound: BX430
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Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay
Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay
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[PMID: 31532206] |
| HEK293 | IC50 |
500 nM
Compound: 5; BX-430
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Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells at -60 mv holding potential by Whole cell patch-clamp method
Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells at -60 mv holding potential by Whole cell patch-clamp method
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[PMID: 31746599] |
| HEK293 | IC50 |
780 nM
Compound: 5; BX-430
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Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells assessed as inhibition of ATP-induced calcium influx by Fluo2-AM staining based inverted fluorescence microscopic method
Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells assessed as inhibition of ATP-induced calcium influx by Fluo2-AM staining based inverted fluorescence microscopic method
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[PMID: 31746599] |
BX430 has virtually no functional impact on all other P2X subtypes (P2X1-P2X3, P2X5, and P2X7)[1].
BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs[1].
Human P2X4-expressing cells treated with thapsigargin plus BX430 shows a significant reduction in the intracellular calcium rise evoked by ATP[1].
BX430 (5 μM) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 688309-70-8
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Appearance Solid
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Masse moléculaire 413.11
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Formule C15H15Br2N3O
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CN=C1)NC2=C(Br)C=C(C(C)C)C=C2Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 83.33 mg/mL (201.71 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 (5.03 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 (5.03 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.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ase AR, et al. Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels. Mol Pharmacol. 2015 Apr;87(4):606-16. [Content Brief]
[2]. Sophocleous RA, et al. Pharmacological and genetic characterisation of the canine P2X4 receptor. Br J Pharmacol. 2020 Feb 4. [Content Brief]
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 | 2.4207 mL | 12.1033 mL | 24.2066 mL | 60.5166 mL |
| 5 mM | 0.4841 mL | 2.4207 mL | 4.8413 mL | 12.1033 mL | |
| 10 mM | 0.2421 mL | 1.2103 mL | 2.4207 mL | 6.0517 mL | |
| 15 mM | 0.1614 mL | 0.8069 mL | 1.6138 mL | 4.0344 mL | |
| 20 mM | 0.1210 mL | 0.6052 mL | 1.2103 mL | 3.0258 mL | |
| 25 mM | 0.0968 mL | 0.4841 mL | 0.9683 mL | 2.4207 mL | |
| 30 mM | 0.0807 mL | 0.4034 mL | 0.8069 mL | 2.0172 mL | |
| 40 mM | 0.0605 mL | 0.3026 mL | 0.6052 mL | 1.5129 mL | |
| 50 mM | 0.0484 mL | 0.2421 mL | 0.4841 mL | 1.2103 mL | |
| 60 mM | 0.0403 mL | 0.2017 mL | 0.4034 mL | 1.0086 mL | |
| 80 mM | 0.0303 mL | 0.1513 mL | 0.3026 mL | 0.7565 mL | |
| 100 mM | 0.0242 mL | 0.1210 mL | 0.2421 mL | 0.6052 mL |
BX430 Related Classifications
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