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Duloxetine

Catalog No. T7061   CAS 116539-59-4

Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder.

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Duloxetine Chemical Structure
Duloxetine, CAS 116539-59-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 40.00
10 mg In stock $ 57.00
25 mg In stock $ 94.00
50 mg In stock $ 139.00
100 mg In stock $ 198.00
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Purity: 99.75%
Purity: 99.31%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder.
Targets&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[1].
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[1].
Molecular Weight 297.41
Formula C18H19NOS
CAS No. 116539-59-4

Storage

store at low temperature,store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 15mg/mL(50.4 mM)

TargetMolReferences and Literature

1. Wang, S.Y., J. Calderon, and G. Kuo Wang, Block of neuronal Na+ channels by antidepressant duloxetine in a state-dependent manner. Anesthesiology, 2010. 113(3): p. 655-65. 2. Ekram, A, R,et al. Duloxetine in Painful Diabetic Neuropathy: A Systematic Review[J]. Clinical Journal of Pain, 2016.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Pediatric Drug Library FDA-Approved Drug Library Antidepressant Compound Library Human Metabolite Library Bioactive Compound Library Neuronal Signaling Compound Library

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Keywords

Duloxetine 116539-59-4 Neuroscience Serotonin Transporter disorder depressive (S)-Duloxetine SERT anxiety inhibit SLC6A4 Inhibitor musculoskeletal LY-248686 generalized pain LY 248686 5-HTT osteoarthiritis LY248686 inhibitor

 

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