TB5

SKU: orb1304016

Description

TB5 is a reversible, selective, and potent inhibitor of human monoamine oxidase B (hMAO-B). This compound is a valuable research tool for investigating MAO-B's role in neurological models, both in cellular assays and animal studies related to Parkinson's disease and other disorders.

Research Area

Metabolism Research, Neuroscience

Key Properties

• CAS Number: 948841-07-4
• MW: 336.25
• Purity: 99.82%
• Formula: C₁₅H₁₄BrNOS
• SMILES: CN(C)c1ccc(\C=C\C(=O)c2ccc(Br)s2)cc1
• Target: Monoamine Oxidase,MAO
• Solubility: DMSO:55 mg/mL (163.57 mM)

Bioactivity

• Target IC50:
  MAO-B (human):0.11±0.01 μM. (Ki)
• In Vivo:
  Compounds are initially dissolved in DMSO (5 mg/mL), then further diluted with a PBS/EtOH mixture (70:30). To elucidate the critical interactions dictating selectivity and potency, kinetic analyses of TB5 and TB8 are conducted. Lineweaver–Burk plots, a total of five, are created to compare the catalytic rates of MAO-B and MAO-A at various substrate concentrations (0.1-1 μM) in both the absence and presence of TB5 and TB8 at differing concentrations. The initial plot reveals the baseline enzyme activity without inhibitors, while the subsequent four plots show the impact of varying concentrations of TB5 and TB8.
• In Vitro:
  TB5 and TB8 interact competitively with the catalytic sites of hMAO-B and hMAO-A. TB5 shows the highest inhibitory activity and selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01 μM and 13.18, respectively. Inhibition by TB5 (hMAO-B) and TB8 (hMAO-A) is fully reversible after 24 hours of dialysis. Cytotoxicity studies reveal TB5 is non-toxic at 5 and 25 μM, with cell viabilities of 95.75% and 84.59%, respectively .
• Cell Research:
  In vitro cytotoxicity of brominated thiophene chalcones and standard MAO inhibitors are tested in human HepG2 hepatic cancer cells at three different concentrations (1, 5 and 25 μM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MonoamineOxidase, Monoamine Oxidase, inhibit, Inhibitor, hMAO-B, MAO, TB 5, TB5, TB-5

Compound Identifiers

PubChem CID

101571768