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Duloxetine [116539-59-4]

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Katalog-Nummer NB-64-38666-1ml

Size : 1mLx10mM(inDMSO)

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Telefonnummer : +1 850 650 7790

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Duloxetine

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Synonyms:

Catalog No. T7061 Copy Product Info

Purity: 99.89%

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

Cas No. 116539-59-4

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.89%

Color:Yellow

Product Introduction

Bioactivity

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].

Chemical Properties

Molecular Weight	297.41
Formula	C₁₈H₁₉NOS
Cas No.	116539-59-4
Smiles	CNCC[C@H](Oc1cccc2ccccc12)c1cccs1
Relative Density.	1.158 g/cm3

Storage & Solubility Information

Storage

Store under nitrogen,Store at low temperature,High Volatility Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (134.49 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 4 mg/mL (13.45 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3624 mL	16.8118 mL	33.6236 mL	168.1181 mL
5 mM	0.6725 mL	3.3624 mL	6.7247 mL	33.6236 mL
10 mM	0.3362 mL	1.6812 mL	3.3624 mL	16.8118 mL
20 mM	0.1681 mL	0.8406 mL	1.6812 mL	8.4059 mL
50 mM	0.0672 mL	0.3362 mL	0.6725 mL	3.3624 mL
100 mM	0.0336 mL	0.1681 mL	0.3362 mL	1.6812 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SLC6A4SERTSerotoninTransporterserotonin-norepinephrine reuptakeSerotonin TransporterpainosteoarthiritismusculoskeletalLY-248686LY248686LY 248686InhibitorinhibitgeneralizedDuloxetinedisorderdepressiveanxiety5-HTT(S)-Duloxetine

Related Tags: Duloxetine chemical structure | Duloxetine in vitro | Duloxetine formula | Duloxetine molecular weight