| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Duloxetine ((S)-Duloxetine; LY248686; LY-248686) is a serotonin-norepinephrine reuptake inhibitor (SNRI, Ki = 4.6 nM) used for treatment of major depressive disorder and generalized anxiety disorder (GAD), fibromyalgia and neuropathic pain.
| Targets |
serotonin reuptake; norepinephrine reuptake
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|---|---|
| ln Vitro |
Duloxetine is a pretreat of norepinephrine reuptake and serotonin (5-HT). Duloxetine has a weaker inhibitory effect on dopamine reuptake when compared to its effects on 5-HT and norepinephrine reuptake. It also exhibits low binding affinity for other neurotransmitter receptors, such as opioid receptors, dopamine D2 receptors, adrenergic, muscarinic (nonselective), and histamine H1 receptors. More than 90% of duloxetine in human plasma is protein bound, according to in vitro research. A1-acid glycoprotein and albumin are the main targets of the binding[1].
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| ln Vivo |
Maximum plasma concentration (Cmax) of duloxetine ranges from about 47 ng/mL (40 mg twice-daily dose) to 110 ng/mL (80 mg twice-daily dose) about 6 hours after dosing. Duloxetine has an elimination half-life of roughly 10–12 hours and a distribution volume of about 1640 L. After a 60 mg single dose, the absolute oral bioavailability ranged from 30% to 80% on average in one study and from 19% to 71% on average in another. Duloxetine absorption is influenced by food and time of day; food and bedtime administration cause a 4-hour tmax delay[1].
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| References |
| Molecular Formula |
C18H19NOS
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|---|---|
| Molecular Weight |
297.416
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| Exact Mass |
297.12
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| CAS # |
116539-59-4
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| Related CAS # |
Duloxetine hydrochloride; 136434-34-9; Duloxetine-d7; 919514-01-5; (±)-Duloxetine hydrochloride; 947316-47-4; Duloxetine metabolite Para-Naphthol Duloxetine; 949095-98-1
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| SMILES |
CNCC[C@@H](C1=CC=CS1)OC2=CC=CC3=CC=CC=C32
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| InChi Key |
ZEUITGRIYCTCEM-KRWDZBQOSA-N
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| InChi Code |
InChI=1S/C18H19NOS/c1-19-12-11-17(18-10-5-13-21-18)20-16-9-4-7-14-6-2-3-8-15(14)16/h2-10,13,17,19H,11-12H2,1H3/t17-/m0/s1
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| Chemical Name |
(3S)-N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-ylpropan-1-amine
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| Synonyms |
LY248686; LY-227942; LY-248686; LY 227942; (S)-Duloxetine; Duloxetine
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3622 mL | 16.8112 mL | 33.6225 mL | |
| 5 mM | 0.6724 mL | 3.3622 mL | 6.7245 mL | |
| 10 mM | 0.3362 mL | 1.6811 mL | 3.3622 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05267873 | Active Recruiting |
Drug: Duloxetine, Vortioxetine | Depressive Disorder, Major | Johns Hopkins Bloomberg School of Public Health |
January 1, 2015 | N/A |
| NCT05930912 | Active Recruiting |
Drug: sertraline 50mg Drug: Duloxetine 20 MG |
PTSD OCD Grief Anxiety Disorders |
Yang I. Pachankis, PhD | June 1, 2023 | N/A |
| NCT04316702 | Active Recruiting |
Device: Hyperbaric oxygen therapy Drug: Cymbalta / lyrica |
Fibromyalgia Emotional Trauma |
Assaf-Harofeh Medical Center | March 1, 2020 | Not Applicable |
| NCT05086393 | Recruiting | Drug: Duloxetine Drug: Placebos |
Pain, Postoperative Total Knee Arthroplasty |
Rush University Medical Center | November 1, 2021 | Phase 4 |
| NCT05510856 | Recruiting | Other: Duloxetine Other: Gabapentin Other: Lacosamide |
Oncology | Tanta University | September 1, 2022 | Phase 4 |
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