PBT434
Based on 2 publication(s) in Google Scholar
PBT434 is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 has the potential for the research of Parkinson’s disease (PD).
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- Purity: 98.86%
- CAS No.: 1232841-78-9
- 화학식: C12H14BrCl2N3O2
- 분자량:383.07
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PBT434
MoreAll α-synuclein Isoforms
More
Biological Activity
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α-synuclein Aggregation |
PBT434 (0-20 µM; 3 h) significantly inhibits H2O2 production by iron and significantly reduces the rate of Fe-mediated aggregation of α-synuclein[1].
PBT434 (0-100 µM; 24 h) shows no cytotoxic effects on brain microvascular endothelial cells[2].
PBT434 (20 µM; 24 h) incrases the expression of total TfR, Cp protein level in hBMVEC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hBMVEC
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Concentration:1, 10, 20, 50, 100 µM
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Incubation Time:24 h
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Result:Showed no cytotoxic effects on brain microvascular endothelial cells.
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Cell Line:hBMVEC
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Concentration:20 μM
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Incubation Time:24 h
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Result:Increased the expression of total TfR, Cp protein level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
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Dosage:30 mg/kg
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Administration:P.o.; daily for 21 days (commencing 3 days following induction of lesion)
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Result:Prevented neuronal loss following 6-OHDA, preserving up to 75% of the SNpc neurons remaining (both Nissl and tyrosine hydroxylase (TH) positive neurons) after the initial phase of cell death.
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Animal Model:12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
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Dosage:1, 3, 10, 30, 80 mg/kg
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Administration:P.o.; daily for 21 days (commenced 24 h after induction of lesion)
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Result:Increased the proportion of SNpc cells rescued, increased there was a trend to improved turning behavior, significantly increased varicosity abundance, prevented the decline in levels of the presynaptic marker synaptophysin (SYNP) in a dose-dependent manner.
Chemical Information
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CAS No. 1232841-78-9
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Appearance Solid
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분자량 383.07
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화학식 C12H14BrCl2N3O2
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Color White to off-white
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SMILES
O=C1N(C)C(CNCC)=NC2=C1C(Cl)=CC(Cl)=C2O.Br
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Synonyms
ATH434
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Metallomics
2024 Oct 4;16(10):mfae044. PMID: 39317669 -
용액&용해도
DMSO : 100 mg/mL (261.05 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (6.53 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.53 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (279 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]. Finkelstein DI, et al. The novel compound PBT434 prevents iron mediated neurodegeneration and alpha-synuclein toxicity in multiple models of Parkinson's disease. Acta Neuropathol Commun. 2017 Jun 28;5(1):53. [Content Brief]
[2]. Bailey DK, Clark W, Kosman DJ. The iron chelator, PBT434, modulates transcellular iron trafficking in brain microvascular endothelial cells. PLoS One. 2021 Jul 26;16(7):e0254794. [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 (sealed storage, away from moisture). 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 | 2.6105 mL | 13.0524 mL | 26.1049 mL | 65.2622 mL |
| 5 mM | 0.5221 mL | 2.6105 mL | 5.2210 mL | 13.0524 mL | |
| 10 mM | 0.2610 mL | 1.3052 mL | 2.6105 mL | 6.5262 mL | |
| 15 mM | 0.1740 mL | 0.8702 mL | 1.7403 mL | 4.3508 mL | |
| 20 mM | 0.1305 mL | 0.6526 mL | 1.3052 mL | 3.2631 mL | |
| 25 mM | 0.1044 mL | 0.5221 mL | 1.0442 mL | 2.6105 mL | |
| 30 mM | 0.0870 mL | 0.4351 mL | 0.8702 mL | 2.1754 mL | |
| 40 mM | 0.0653 mL | 0.3263 mL | 0.6526 mL | 1.6316 mL | |
| 50 mM | 0.0522 mL | 0.2610 mL | 0.5221 mL | 1.3052 mL | |
| 60 mM | 0.0435 mL | 0.2175 mL | 0.4351 mL | 1.0877 mL | |
| 80 mM | 0.0326 mL | 0.1632 mL | 0.3263 mL | 0.8158 mL | |
| 100 mM | 0.0261 mL | 0.1305 mL | 0.2610 mL | 0.6526 mL |
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