2. Neuronal Signaling
  3. α-synuclein
  4. PBT434

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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PBT434 Chemical Structure

PBT434 Chemical Structure

CAS No. : 1232841-78-9

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Based on 1 publication(s) in Google Scholar

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PBT434 Related Antibodies

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α-synuclein α-synuclein Aggregation α-synuclein/CHMP2B

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  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1].

IC50 & Target

α-synuclein Aggregation

 

In Vitro

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.

PBT434 Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: hBMVEC
Concentration: 1, 10, 20, 50, 100 µM
Incubation Time: 24 h
Result: Showed no cytotoxic effects on brain microvascular endothelial cells.

Western Blot Analysis[2]

Cell Line: hBMVEC
Concentration: 20 μM
Incubation Time: 24 h
Result: Increased the expression of total TfR, Cp protein level.
In Vivo

PBT434 (30 mg/kg; p.o.; daily for 21 days) significantly preserved neuron numbers in the 6-OHDA intoxication model and shows significantly fewer rotations in the L-DOPA model, significantly reducing SNpc neuronal loss in the MPTP model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
Dosage: 30 mg/kg
Administration: P.o.; daily for 21 days (commencing 3 days following induction of lesion)
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.
Animal Model: 12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
Dosage: 1, 3, 10, 30, 80 mg/kg
Administration: P.o.; daily for 21 days (commenced 24 h after induction of lesion)
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.
Clinical Trial
Molecular Weight

383.07

Formula

C12H14BrCl2N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C)C(CNCC)=NC2=C1C(Cl)=CC(Cl)=C2O.Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6105 mL 13.0524 mL 26.1049 mL
5 mM 0.5221 mL 2.6105 mL 5.2210 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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 2.6105 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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PBT434 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PBT4341232841-78-9ATH434PBT 434PBT-434ATH 434ATH-434α-synucleinα-Synorally activecross the blood-brain barrierSNpcironParkinson’s diseaseInhibitorinhibitorinhibit

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