Duloxetine

SKU: orb1300102

Description

Duloxetine

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 116539-59-4
• MW: 297.41
• Purity: 99.89% (May vary between batches)
• Formula: C₁₈H₁₉NOS
• SMILES: CNCC[C@H](Oc1cccc2ccccc12)c1cccs1
• Target: Serotonin Transporter
• Solubility: DMSO:40 mg/mL (134.49 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:4 mg/mL (13.45 mM)

Bioactivity

• Target IC50:
  5-HT-Norepinephrine reuptake:4.6 nM(ki)
• In Vitro:
  IC50 of duloxetine for the resting and inactivated wild-type hNav1.7 Na+ channel were 22.1+/-0.4 and 1.79+/-0.10 microM, respectively (mean+/-SE, n=5). The IC50 for the open Na+ channel was 0.25+/-0.02 microM (n=5), as determined by the block of persistent late Nav1.7 Na+ currents. Similar open-channel block by duloxetine was found in the muscle Nav1.4 isoform (IC50=0.51+/-0.05 microM; n=5). Block by duloxetine appeared via the conserved local anesthetic receptor as determined by site-directed mutagenesis. Finally, duloxetine elicited strong use-dependent block of neuronal transient Nav1.7 Na+ currents during repetitive stimulations.
• Cell Research:
  Used the whole cell, patch clamp technique to test whether duloxetine interacts with the neuronal Nav1.7 Na+ channel as a potential target. Resting and inactivated Nav1.7 Na+ channel block by duloxetine were measured by conventional pulse protocols in transfected human embryonic kidney cells. The open-channel block was determined directly using inactivation-deficient mutant Nav1.7 Na+ channels.

Storage & Handling

• Storage: store at low temperature,store under nitrogen | Pure form: -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

pain, LY248686, LY-248686, LY 248686, musculoskeletal, inhibit, Inhibitor, generalized, 5-HTT, (S)-Duloxetine, anxiety, depressive, Duloxetine, disorder, SLC6A4, SERT, osteoarthiritis, Serotonin Transporter, serotonin-norepinephrine reuptake, SerotoninTransporter

Compound Identifiers

PubChem CID

60835