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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
Iron-generated H2O2 is greatly inhibited and the rate of Fe-mediated α-synuclein aggregation is significantly reduced by PBT434 methanesulfonate (0–20 µM; 3 hours) [1]. Brain microvascular endothelial cells are not cytotoxically affected by PBT434 methanesulfonate (0-100 µM; 24 h) [2]. The expression of total TfR and Cp protein levels in hBMVEC is increased by PBT434 methanesulfonate (20 µM; 24 h) [2].
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ln Vivo |
PBT434 methanesulfonate (30 mg/kg; oral; once daily for 21 days) demonstrated considerably less rotation in the L-DOPA paradigm, greatly reduced SNpc neuron loss in the MPTP model, and significantly conserved neuronal number in the 6-OHDA toxicity model[1].
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Cell Assay |
Cell Cytotoxicity Assay[2]
Cell Types: hBMVEC Tested Concentrations: 1, 10, 20, 50, 100 µM Incubation Duration: 24 h Experimental Results: demonstrated no cytotoxic effects on brain microvascular endothelial cells. Western Blot Analysis[2] Cell Types: hBMVEC Tested Concentrations: 20 μM Incubation Duration: 24 h Experimental Results: Increased the expression of total TfR, Cp protein level. |
Animal Protocol |
Animal/Disease Models: 12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
Doses: 30 mg/kg Route of Administration: Po; daily for 21 days (commencing 3 days following induction of lesion) Experimental Results: 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/Disease Models: 12 weeks, 25 g, Male C57BL/ 6 J mice (MPTP model)[1] Doses: 1, 3, 10, 30, 80 mg/kg Route of Administration: Po; daily for 21 days (commenced 24 h after induction of lesion) Experimental Results: Increased the proportion of SNpc cells rescued , increased there was a trend to improved turning behavior, Dramatically increased varicosity abundance, prevented the decline in levels of the presynaptic marker synaptophysin (SYNP) in a dose-dependent manner. |
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.
[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. |
Molecular Formula |
C13H17CL2N3O5S
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Molecular Weight |
398.26
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CAS # |
2387898-69-1
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SMILES |
S(O)(=O)(=O)C.O=C1N(C(CNCC)=NC2=C(C(Cl)=CC(Cl)=C12)O)C
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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)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 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 | |
10 mM | 0.2511 mL | 1.2555 mL | 2.5109 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.