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

PBT434 mesylate  (Synonyms: ATH434 mesylate)

Cat. No.: HY-120475A Purity: 99.74%
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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.

PBT434 mesylate Chemical Structure

PBT434 mesylate Chemical Structure

CAS No. : 2387898-69-1

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10 mg USD 1550 In-stock
25 mg USD 3100 In-stock
50 mg USD 4980 In-stock
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Based on 1 publication(s) in Google Scholar

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PBT434 mesylate Related Antibodies

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Description

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)[1][2].

In Vitro

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.

PBT434 mesylate 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 methanesulfonate (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 (MPTP 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.
Molecular Weight

398.26

Formula

C13H17Cl2N3O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N=C(CNCC)N1C)C(O)=C(Cl)C=C2Cl.O=S(O)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5109 mL 12.5546 mL 25.1092 mL
5 mM 0.5022 mL 2.5109 mL 5.0218 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 (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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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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 (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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PBT434 mesylate 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:

PBT4342387898-69-1ATH434PBT 434PBT-434ATH 434ATH-434α-synucleinα-Synorally activecross the blood-brain barrierSNpcironParkinson’s diseaseInhibitorinhibitorinhibit

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