Cat. No.: HY-B0161

Duloxetine

(Synonyms: LY248686)

12 Cited Publications

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Based on 12 publication(s) in Google Scholar

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).

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Pureté: 99.92%
CAS No.: 116539-59-4
Formule: C₁₈H₁₉NOS
Masse moléculaire:297.41

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Duloxetine Chemical Structure

CAS No.: 116539-59-4

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Publications (12)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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	>1000 nM Compound: 2	Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes	[PMID: 20378347]
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	19 nM Compound: duloxetine	Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells	[PMID: 16750359]
HEK293	IC₅₀	6 nM Compound: duloxetine	Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells	[PMID: 16750359]
HEK293	IC₅₀	870 nM Compound: duloxetine	Inhibition of DA transporter expressed in HEK293 cells Inhibition of DA transporter expressed in HEK293 cells	[PMID: 16750359]
HEK293	IC₅₀	19 nM Compound: duloxetine	Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells	[PMID: 16750363]
HEK293	IC₅₀	6 nM Compound: duloxetine	Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells	[PMID: 16750363]
HEK293	IC₅₀	870 nM Compound: duloxetine	Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells	[PMID: 16750363]
HEK293	IC₅₀	19 nM Compound: duloxetine	Inhibition of [3H]NA from human NET expressed in HEK293 cells Inhibition of [3H]NA from human NET expressed in HEK293 cells	[PMID: 17267217]
HEK293	IC₅₀	6 nM Compound: duloxetine	Inhibition of [3H]5-HT from human SERT expressed in HEK293 cells Inhibition of [3H]5-HT from human SERT expressed in HEK293 cells	[PMID: 17267217]
HEK293	IC₅₀	870 nM Compound: duloxetine	Inhibition of [3H]DA from human DAT expressed in HEK293 cells Inhibition of [3H]DA from human DAT expressed in HEK293 cells	[PMID: 17267217]
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	4 nM Compound: 2	Inhibition of [3H]5-HT uptake at human 5HTT expressed in HEK293 cells Inhibition of [3H]5-HT uptake at human 5HTT expressed in HEK293 cells	[PMID: 19359175]
HEK293	IC₅₀	5 nM Compound: 2	Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells	[PMID: 19359175]
HEK293	IC₅₀	590 nM Compound: 2	Inhibition of [3H]DA uptake at human DAT expressed in HEK293 cells Inhibition of [3H]DA uptake at human DAT expressed in HEK293 cells	[PMID: 19359175]
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	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	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	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]
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	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	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]
JAR	IC₅₀	3 nM Compound: 3	Inhibition of serotonin uptake at human SERT expressed in JAR cells Inhibition of serotonin uptake at human SERT expressed in JAR cells	[PMID: 18771916]
JAR	IC₅₀	3 nM Compound: 5	Inhibition of serotonin uptake at human SERT expressed in human JAR cells Inhibition of serotonin uptake at human SERT expressed in human JAR cells	[PMID: 19329313]
JAR	IC₅₀	3 nM Compound: 2	Inhibition of human SERT expressed in human JAR cells Inhibition of human SERT expressed in human JAR cells	[PMID: 20378347]
MDCK	IC₅₀	4 nM Compound: 3	Inhibition of norepinephrine uptake at human NET expressed in MDCK cells Inhibition of norepinephrine uptake at human NET expressed in MDCK cells	[PMID: 18771916]

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 116539-59-4
Appearance Oil
Masse moléculaire 297.41
Formule C₁₈H₁₉NOS
Color Light brown to yellow
SMILES

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

LY248686
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (12)

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Journal Impact Factor

Cell

Unveiling conformation-selective regulation of the norepinephrine transporter. [Abstract]

2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730
Autophagy

Duloxetine ameliorates cerebral ischemic injury by inhibiting autophagy. [Abstract]

2026 Mar 5. PMID: 41787744

Duloxetine purchased from MedChemExpress. Usage Cited in: Autophagy. 2026 Mar 5. [Abstract]

Duloxetine hydrochloride (Duloxetine Hcl; 10 μM; 15 h) increased LC3-II levels incubated neurons in a nutrient-limited medium (nutrient deprivation, ND).

Duloxetine purchased from MedChemExpress. Usage Cited in: Autophagy. 2026 Mar 5. [Abstract]

Duloxetine hydrochloride (Dulox.; 10 μM; 15 h) showed the average number of LAMP1+ puncta did not change in response to these treatments, we observed a significant swelling of LAMP1+ vesicles in Neuro-2a cells.

Duloxetine purchased from MedChemExpress. Usage Cited in: Autophagy. 2026 Mar 5. [Abstract]

Duloxetine hydrochloride (Dulox.; 10 μM; 15 h) induced enlargement of the lysosome in Neuro-2a cells.
Phytomedicine

Huangqi Guizhi Wuwu decoction alleviate Oxaliplatin-Induced Peripheral Neuropathy by adjusting the myelin regeneration. [Abstract]

2025 Sep:145:157039. PMID: 40618490
Cell Chem Biol

Suppression of pain transmission and behavior by inhibition of peripheral diacylglycerol metabolism. [Abstract]

2026 Jan 15;33(1):74-90.e19. PMID: 41544618
Eur J Pharmacol

L1CAM mimetic compound duloxetine improves cognitive impairment in 5xFAD mice and protects Aβ1-42-damaged HT22 cells. [Abstract]

2025 Jun 15:997:177476. PMID: 40057157
Pharmacol Rep

Therapeutic potential of combining mirogabalin with antidepressants in relieving hypersensitivity: evidence from a mouse model of neuropathic pain. [Abstract]

2026 May 28. PMID: 42207469
Autism Res

Duloxetine ameliorates valproic acid-induced hyperactivity, anxiety-like behavior, and social interaction deficits in zebrafish. [Abstract]

2022 Jan;15(1):27-41. PMID: 34605202
Neurotox Res

Duloxetine-Induced Neural Cell Death and Promoted Neurite Outgrowth in N2a Cells. [Abstract]

2020 Dec;38(4):859-870. PMID: 32415528

Duloxetine purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2020 Dec;38(4):859-870. [Abstract]

Duloxetine hydrochloride (Duloxetine; 0-100 μM; 24 h) inhibited cell viability in N2a cells (a) and C17.2 cells (b).

Duloxetine purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2020 Dec;38(4):859-870. [Abstract]

Duloxetine hydrochloride (Duloxetine; 0, 12.5, 25, 50, 100 μM; 24 h) inhibited N2a cells and C17.2 cells viability in a dose-dependent manner.

Duloxetine purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2020 Dec;38(4):859-870. [Abstract]

Duloxetine hydrochloride (Duloxetine; 0, 12.5, 25, 50, 100 μM; 24 h) inhibited N2a viability in a dose-dependent manner.
Mol Brain

Target oxidative stress-induced disulfidptosis: novel therapeutic avenues in Parkinson's disease. [Abstract]

2025 Apr 4;18(1):29. PMID: 40186271
Neurosci Lett

Participation of transient receptor potential vanilloid 1 in the analgesic effect of duloxetine for paclitaxel induced peripheral neuropathic pain. [Abstract]

2022 Mar 16;773:136512. PMID: 35149198
Patent

US20250002569A1.
Università Vita-Salute San Raffaele

2022 Apr 08. 34.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (336.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3624 mL

16.8118 mL

33.6236 mL

5 mM

0.6725 mL

3.3624 mL

6.7247 mL

10 mM

0.3362 mL

1.6812 mL

3.3624 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (16.81 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (16.81 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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+
%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3624 mL	16.8118 mL	33.6236 mL	84.0590 mL
	5 mM	0.6725 mL	3.3624 mL	6.7247 mL	16.8118 mL
	10 mM	0.3362 mL	1.6812 mL	3.3624 mL	8.4059 mL
	15 mM	0.2242 mL	1.1208 mL	2.2416 mL	5.6039 mL
	20 mM	0.1681 mL	0.8406 mL	1.6812 mL	4.2030 mL
	25 mM	0.1345 mL	0.6725 mL	1.3449 mL	3.3624 mL
	30 mM	0.1121 mL	0.5604 mL	1.1208 mL	2.8020 mL
	40 mM	0.0841 mL	0.4203 mL	0.8406 mL	2.1015 mL
	50 mM	0.0672 mL	0.3362 mL	0.6725 mL	1.6812 mL
	60 mM	0.0560 mL	0.2802 mL	0.5604 mL	1.4010 mL
	80 mM	0.0420 mL	0.2101 mL	0.4203 mL	1.0507 mL
	100 mM	0.0336 mL	0.1681 mL	0.3362 mL	0.8406 mL

Keywords

Duloxetine

12 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Duloxetine

Activité biologique

Chemical Information

Publications (12)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Duloxetine Related Classifications

HY-B0161 Related Classifications