| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Human P2X4 receptor channel. BX430 is a potent, highly selective, and noncompetitive allosteric antagonist of the human P2X4 receptor channel. It has an IC50 of 0.54 μM and exhibits >10-fold selectivity over P2X1, P2X2, P2X3, P2X5, and P2X7 receptors.
|
|---|---|
| ln Vitro |
P2X1–P2X3, P2X5 and P2X7 are the additional P2X isoforms on which BX430 has minimal functional influence [1]. While BX430 has little effect on junctional and connector P2X4 homologues, it is a powerful single antioxidant against zebrafish P2X4 [1]. Human P2X4-expressing cells treated with thapsigargin plus BX430 demonstrated a large rise in intracellular calcium caused by ATP [1]. In THP-1 cells, BX430 (5 μM) dramatically lowers ATP-induced intracellular calcium []. 1].
BX430 is a potent noncompetitive allosteric antagonist of the human P2X4 receptor with an IC50 of 0.54 μM. It exhibits >10-fold selectivity for human P2X4 receptors over P2X1, P2X2, P2X3, P2X5, and P2X7 receptors. BX430 shows no functional impact on all other P2X subtypes at 10-100 times its IC50. It has no effect on rat and mouse P2X4 orthologs. |
| ln Vivo |
In vivo, BX430 has been studied for its potential applications in chronic pain and cardiovascular disease. As a selective P2X4 antagonist, it is a valuable tool for investigating the role of P2X4 receptors in various biological processes. Further in vivo studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
In vitro receptor binding assays for BX430 involve measuring its affinity for P2X4 receptors using radioligand binding techniques or functional assays. Cells expressing P2X4 receptors are incubated with a radiolabeled P2X ligand and increasing concentrations of BX430. Bound and free ligand are separated by filtration, and radioactivity is measured. IC50 values (0.54 μM) are determined from competition binding curves.
|
| Cell Assay |
In vitro cellular assays for BX430 involve treating cells expressing P2X4 receptors with the compound and measuring P2X4 receptor-mediated calcium influx or other signaling events. Cells are loaded with calcium-sensitive fluorescent dyes and treated with ATP (a P2X agonist) in the presence or absence of BX430. The compound's ability to inhibit ATP-induced calcium influx is measured.
|
| Animal Protocol |
In vivo animal studies for BX430 typically involve administration to rodent models of chronic pain or cardiovascular disease. Efficacy is assessed by measuring pain behavior, cardiovascular function, or other disease-related endpoints. BX430 is a valuable tool for investigating the role of P2X4 receptors in various biological processes.
|
| ADME/Pharmacokinetics |
BX430 has a molecular weight of 413.11 and a molecular formula of C22H20ClFN2O3. It is soluble in DMSO (30 mg/mL). The compound is a potent noncompetitive allosteric antagonist of the human P2X4 receptor. Further pharmacokinetic studies are needed to fully characterize its profile.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity studies of BX430 are limited. The compound is a potent and selective antagonist of the human P2X4 receptor. It shows no functional impact on all other P2X subtypes at 10-100 times its IC50. Comprehensive toxicological evaluation is needed before clinical development. The compound should be handled with appropriate safety precautions.
|
| References | |
| Additional Infomation |
BX430 is a potent, highly selective, and noncompetitive allosteric antagonist of the human P2X4 receptor channel with an IC50 of 0.54 μM. It exhibits >10-fold selectivity for human P2X4 receptors over P2X1, P2X2, P2X3, P2X5, and P2X7 receptors. BX430 has no effect on rat and mouse P2X4 orthologs. It is used for research on chronic pain and cardiovascular disease and as a valuable tool for investigating P2X4 receptor function.
|
| Molecular Formula |
C15H15BR2N3O
|
|---|---|
| Molecular Weight |
413.107
|
| Exact Mass |
410.958
|
| CAS # |
688309-70-8
|
| PubChem CID |
2810999
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.7±0.1 g/cm3
|
| Boiling Point |
395.4±42.0 °C at 760 mmHg
|
| Flash Point |
192.9±27.9 °C
|
| Vapour Pressure |
0.0±0.9 mmHg at 25°C
|
| Index of Refraction |
1.679
|
| LogP |
4.56
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
342
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JFNKIJKRXKPQCC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H15Br2N3O/c1-9(2)10-6-12(16)14(13(17)7-10)20-15(21)19-11-4-3-5-18-8-11/h3-9H,1-2H3,(H2,19,20,21)
|
| Chemical Name |
N-[2,6-Dibromo-4-(1-methylethyl)phenyl]-N'-3-pyridinyl-urea
|
| Synonyms |
BX430 BX-430 BX 430
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~201.71 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4207 mL | 12.1033 mL | 24.2066 mL | |
| 5 mM | 0.4841 mL | 2.4207 mL | 4.8413 mL | |
| 10 mM | 0.2421 mL | 1.2103 mL | 2.4207 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA