PBT434 mesylate
Based on 2 publication(s) in Google Scholar
PBT434 methanesulfonate is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 methanesulfonate can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 methanesulfonate inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 methanesulfonate prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 methanesulfonate has the potential for the research of Parkinson’s disease (PD).
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 2387898-69-1
- Formula: C13H17Cl2N3O5S
- Molecular Weight:398.26
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Storage:
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PBT434 mesylate
MoreAll α-synuclein Isoforms
More
Biological Activity
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α-synuclein Aggregation |
PBT434 methanesulfonate (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 methanesulfonate (0-100 µM; 24 h) shows no cytotoxic effects on brain microvascular endothelial cells[2].
PBT434 methanesulfonate (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 (MPTP 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. 2387898-69-1
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Appearance Solid
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Molecular Weight 398.26
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Formula C13H17Cl2N3O5S
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Color White to off-white
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SMILES
O=C1C2=C(N=C(CNCC)N1C)C(O)=C(Cl)C=C2Cl.O=S(O)(C)=O
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Synonyms
ATH434 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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 -
Solvent & Solubility
DMSO : 100 mg/mL (251.09 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)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.5109 mL | 12.5546 mL | 25.1092 mL | 62.7731 mL |
| 5 mM | 0.5022 mL | 2.5109 mL | 5.0218 mL | 12.5546 mL | |
| 10 mM | 0.2511 mL | 1.2555 mL | 2.5109 mL | 6.2773 mL | |
| 15 mM | 0.1674 mL | 0.8370 mL | 1.6739 mL | 4.1849 mL | |
| 20 mM | 0.1255 mL | 0.6277 mL | 1.2555 mL | 3.1387 mL | |
| 25 mM | 0.1004 mL | 0.5022 mL | 1.0044 mL | 2.5109 mL | |
| 30 mM | 0.0837 mL | 0.4185 mL | 0.8370 mL | 2.0924 mL | |
| 40 mM | 0.0628 mL | 0.3139 mL | 0.6277 mL | 1.5693 mL | |
| 50 mM | 0.0502 mL | 0.2511 mL | 0.5022 mL | 1.2555 mL | |
| 60 mM | 0.0418 mL | 0.2092 mL | 0.4185 mL | 1.0462 mL | |
| 80 mM | 0.0314 mL | 0.1569 mL | 0.3139 mL | 0.7847 mL | |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2511 mL | 0.6277 mL |
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