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Duloxetine Serotonin Transporter inhibitor

Name: Duloxetine
Brand: Selleck Chemicals
SKU: S5071
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5071

Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake.

Chemical Structure

Molecular Weight: 297.41

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel GluR MAO Beta Amyloid NMDAR P2 Receptor Trk receptor Notch Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor BChE Adenosine Deaminase CCK receptor MT Receptor

Chemical Information, Storage & Stability

Molecular Weight	297.41	Formula	C₁₈H₁₉NOS	Storage (From the date of receipt)	2 years -20°C liquid
CAS No.	116539-59-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY-248686			Smiles	CNCCC(C1=CC=CS1)OC2=CC=CC3=CC=CC=C32

Solubility

In vitro
Batch:

DMSO : 59 mg/mL ( (198.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.950mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 59 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (5.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	serotonin reuptake ^[1] norepinephrine reuptake ^[1]
In vitro	Duloxetine is a potent inhibitor of serotonin (5-HT) and norepinephrine reuptake. Compared with its effects on 5-HT and norepinephrine reuptake, duloxetine weakly inhibits dopamine reuptake and has low binding affinity for other neurotransmitter receptors, including adrenergic, muscarinic (nonselective) and histamine H1 receptors; dopamine D2 receptors; 5-HT1A, 5-HT1D and 5-HT2C receptors; and opioid receptors. In vitro studies showed that more than 90% of duloxetine is protein bound in human plasma. The binding occurs primarily to albumin and a1-acid glycoprotein^[1].
In vivo	Duloxetine achieves a maximum plasma concentration (Cmax) of approximately 47 ng/mL (40mg twice-daily dosing) to 110 ng/mL (80 mg twice-daily dosing) approximately 6 hours after dosing. The elimination half-life of duloxetine is approximately 10–12 hours and the volume of distribution is approximately 1640 L. The absolute oral bioavailability averaged 50%, ranging from 30% to 80%, after a 60 mg single dose in one study and averaged 43%, ranging from 19% to 71%, in another study. Food and time of day impact duloxetine absorption, with food and bedtime administration delaying tmax by 4 hours^[1].
References	https://pubmed.ncbi.nlm.nih.gov/21366359/

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