Duloxetine (Synonyms: LY248686)

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Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a K_i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Duloxetine hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Duloxetine Chemical Structure

CAS No. : 116539-59-4

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Other In-stock Forms of Duloxetine:

Duloxetine hydrochloride

Other Forms of Duloxetine:

Duloxetine hydrochloride In-stock
Duloxetine-d₇ hydrochloride Get quote
(R)-Duloxetine Get quote
(R)-Duloxetine hydrochloride Get quote
(±)-Duloxetine hydrochloride Get quote
Duloxetine-d₇ Get quote
Duloxetine metabolite Para-Naphthol Duloxetine Get quote

5 Publications Citing Use of MCE Duloxetine

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a K_i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD)^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	2.8 μM Compound: duloxetine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	10.4 nM Compound: duloxetine	Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	[PMID: 25221656]
HEK293	IC₅₀	10.4 nM Compound: Duloxetine	Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	[PMID: 24974340]
HEK293	IC₅₀	2.3 nM Compound: 5	Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis	[PMID: 24900709]
HEK293	IC₅₀	29 nM Compound: 5	Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis	[PMID: 24900709]
HEK293	IC₅₀	515 nM Compound: duloxetine	Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	[PMID: 25221656]
HEK293	IC₅₀	515 nM Compound: Duloxetine	Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	[PMID: 24974340]
HEK293	IC₅₀	6.6 nM Compound: 7	Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter	[PMID: 18954038]
HEK293	IC₅₀	660 nM Compound: 7	Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter	[PMID: 18954038]
HEK293	IC₅₀	8.9 nM Compound: 7	Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter	[PMID: 18954038]
HEK293	IC₅₀	977 nM Compound: duloxetine	Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	[PMID: 25221656]
HEK293	IC₅₀	977 nM Compound: Duloxetine	Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	[PMID: 24974340]

In Vitro

Duloxetine ((S)-Duloxetine) inhibits the reuptake of serotonin and norepinephrine in the central nervous system. Duloxetine is also considered a less potent inhibitor of dopamine reuptake. However, duloxetine has no significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and GABA receptors and can therefore be considered to be a selective reuptake inhibitor at the 5-HT and NA transporters. Duloxetine undergoes extensive metabolism, but the major circulating metabolites do not contribute significantly to the pharmacologic activity. Major depressive disorder is believed to be due in part to an increase in pro-inflammatory cytokines within the central nervous system. Antidepressants including ones with a similar mechanism of action as duloxetine, i.e. serotonin metabolism inhibition, cause a decrease in proinflammatory cytokine activity and an increase in anti-inflammatory cytokines; this mechanism may apply to duloxetine in its effect on depression but research on cytokines specific to duloxetine therapy is lacking^[1].
The analgesic properties of duloxetine in the treatment of diabetic neuropathy and central pain syndromes such as fibromyalgia are believed to be due to sodium ion channel blockade^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

297.41

Formula

C₁₈H₁₉NOS

CAS No.

116539-59-4

SMILES

CNCC[C@H](OC1=CC=CC2=C1C=CC=C2)C3=CC=CS3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. De Berardis, D., et al., The effect of newer serotonin-noradrenalin antidepressants on cytokine production: a review of the current literature. Int J Immunopathol Pharmacol, 2010. 23(2): p. 417-22. [Content Brief]

[2]. 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. [Content Brief]

Duloxetine Related Classifications

Molarity Calculator
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Duloxetine116539-59-4LY248686LY 248686LY-248686Serotonin Transporter5-HTTSERTSLC6A4depressivedisordergeneralizedanxietyosteoarthiritismusculoskeletalpainInhibitorinhibitorinhibit

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