5-BDBD
Based on 4 publication(s) in Google Scholar
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
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- Pureza: 99.96%
- No. CAS: 768404-03-1
- Fòrmula: C17H11BrN2O2
- Peso molecular:355.19
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) 5-BDBD
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RT-PCR
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In Vivo Efficacy Study
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Actividad biológica
Descripciòn
IC50 & Target
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P2X4 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.5 μM
Compound: 5-BDBD
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Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as inhibition of ATP-induced calcium influx
Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as inhibition of ATP-induced calcium influx
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[PMID: 27427902] |
| CHO | IC50 |
500 nM
Compound: 1; 5-BDBD
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Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as reduction in ATP induced calcium influx
Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as reduction in ATP induced calcium influx
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[PMID: 31746599] |
| HEK293 | IC50 |
1.2 μM
Compound: 5-BDBD
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Antagonist activity at human P2X4R transfected in HEK293 cells
Antagonist activity at human P2X4R transfected in HEK293 cells
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[PMID: 31532206] |
| HEK293 | IC50 |
9.2 μM
Compound: 5-BDBD
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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] |
In Vitro
5-BDBD inhibits 10 μM ATP-induced currents of rP2X4R-expressing HEK293 cells in a concentration-dependent manner, with an IC50 of 0.75 μM[1].
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5-BDBD displaces rightward the ATP concentration-response curve, with an EC50 of 4.7 to 15.9 μM[1].
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5-BDBD could be specifically used to discriminate between P2X1R, P2X2aR, P2X2bR, P2X3R, P2X4R, and P2X7R[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice[2]
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Dosage:28 mg/kg
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Administration:I.p.; daily for 9 days
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Result:Prevented NTG-induced mechanical hypersensitivity.
Chemical Information
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No. CAS 768404-03-1
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Appearance Solid
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Peso molecular 355.19
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Fòrmula C17H11BrN2O2
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Color White to light yellow
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SMILES
O=C1CN=C(C2=CC=CC(Br)=C2)C(OC3=CC=CC=C34)=C4N1
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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 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Neural Regen Res
Overexpression of the inwardly rectifying potassium channel Kir4.1 or Kir4.1 Tyr 9 Asp in Müller cells exerts neuroprotective effects in an experimental glaucoma model. [Abstract]2026 Apr 1;21(4):1628-1640. PMID: 39589165
5-BDBD purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2026 Apr 1;21(4):1628-1640. [Abstract]
When microglia were pre-incubated with the P2X7R antagonist A740003 (1 μM) or the P2X4R antagonist 5-BDBD (5 μM), the changes in IL-1β mRNA levels were reversed.
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Cell Mol Life Sci
2022 Aug 16;79(9):483. PMID: 35972649
5-BDBD purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2022 Aug 16;79(9):483. [Abstract]
The positive response rate by the von Frey test at the injury-level segment with a stimulation strength of 0.04 g in allodynia-positive mice (DMSO, n = 4; 5-BDBD (28 mg/kg), n = 6).
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Int Immunopharmacol
Fast green FCF prevents postoperative cognitive dysfunction via the downregulation of the P2X4 receptor in mice. [Abstract]2023 Aug:121:110462. PMID: 37301120 -
J Endocrinol Invest
2025 Feb;48(2):317-332. PMID: 39527372
Solvente y solubilidad
In Vitro:
DMSO : 62.5 mg/mL (175.96 mM; ultrasonic and warming and heat to 60°C; 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)
In Vivo:
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: 15% Solutol HS 15 10% Cremophor EL 35% PEG 400 40% water
Solubility: 9.8 mg/mL (27.59 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.86 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 2 mg/mL (5.63 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
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 (283 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
[1]. Coddou C, et al. Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett. 2019;690:219-224. [Content Brief]
[2]. Long T, et al. Microglia P2X4 receptor contributes to central sensitization following recurrent nitroglycerin stimulation. J Neuroinflammation. 2018;15(1):245. Published 2018 Aug 30. [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, 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 | 2.8154 mL | 14.0770 mL | 28.1539 mL | 70.3849 mL |
| 5 mM | 0.5631 mL | 2.8154 mL | 5.6308 mL | 14.0770 mL | |
| 10 mM | 0.2815 mL | 1.4077 mL | 2.8154 mL | 7.0385 mL | |
| 15 mM | 0.1877 mL | 0.9385 mL | 1.8769 mL | 4.6923 mL | |
| 20 mM | 0.1408 mL | 0.7038 mL | 1.4077 mL | 3.5192 mL | |
| 25 mM | 0.1126 mL | 0.5631 mL | 1.1262 mL | 2.8154 mL | |
| 30 mM | 0.0938 mL | 0.4692 mL | 0.9385 mL | 2.3462 mL | |
| 40 mM | 0.0704 mL | 0.3519 mL | 0.7038 mL | 1.7596 mL | |
| 50 mM | 0.0563 mL | 0.2815 mL | 0.5631 mL | 1.4077 mL | |
| 60 mM | 0.0469 mL | 0.2346 mL | 0.4692 mL | 1.1731 mL | |
| 80 mM | 0.0352 mL | 0.1760 mL | 0.3519 mL | 0.8798 mL | |
| 100 mM | 0.0282 mL | 0.1408 mL | 0.2815 mL | 0.7038 mL |
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