5.30583

α-Synuclein Blocker, ELN484228

• Synonym(s): α-Synuclein Blocker, ELN484228, N-(4-Fluorophenyl)benzenesulfonamide, NSC164389, ELN 484228
• Empirical Formula (Hill Notation): C₁₂H₁₀FNO₂S
• CAS Number: 312-63-0
• Molecular Weight: 251.28
• MDL number: MFCD00091019
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C12H10FNO2S/c13-10-6-8-11(9-7-10)14-17(15,16)12-4-2-1-3-5-12/h1-9,14H
• InChI key: AZORQGXJAXEIGC-UHFFFAOYSA-N

Description

General description

A cell-permeable phenylsulfonamide compound that reversibly binds to pocket I of the monomeric α-synuclein (α-syn) and reverses α-syn-induced impairment of phagocytosis in H4 neuroglioma cells over-expressing wild-type α-syn and microglia isolated from α-syn BAC transgenic animals over-expressing the E46K mutant form of human α-syn (~1-10 µM). Reduces α-syn-mediated impairment of vesicular dynamics and diminishes α-syn translocation to the synaptic region in rat primary neuronal cultures by 50% (at ~ 1 µM) and in cortical cultures in transgenic mice over-expressing human α-syn. Also shown to protect dopaminergic neurons against the toxic effects of over-expressed α-syn A53T and reduces neurite retraction in TH- and MAP2-positive neurons.

A cell-permeable phenylsulfonamide compound that reversibly binds to pocket I of the monomeric α-synuclein (α-syn) and reverses α-syn-induced impairment of phagocytosis in H4 neuroglioma cells over-expressing wild-type α-syn and microglia isolated from α-syn BAC transgenic animals over-expressing the E46K mutant form of human α-syn (~1-10 µM). Reduces α-syn-mediated impairment of vesicular dynamics and diminishes α-syn translocation to the synaptic region in rat primary neuronal cultures by 50% (at ~ 1 µM) and in cortical cultures in transgenic mice over-expressing human α-syn. Also shown to protect dopaminergic neurons against the toxic effects of over-expressed α-syn A53T and reduces neurite retraction in TH- and MAP2-positive neurons.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
monomeric α-synuclein

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Toth, G., et al. 2014. PLoS ONE9, e87133.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Pictograms: GHS07
• Signal Word: Warning
• Hazard Statements: H302 - H319
• Precautionary Statements: P264 - P280 - P301 + P312 - P305 + P351 + P338 - P337 + P313 - P501
• Hazard Classifications: Acute Tox. 4 Oral - Eye Irrit. 2
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable