Dapoxetine HCl

Catalog No.S1869 Synonyms: LY-210448

For research use only.

Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

Dapoxetine HCl  Chemical Structure

CAS No. 129938-20-1

Purity & Quality Control

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Biological Activity

Description Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
Targets
5-HT [1]
In vitro

Dapoxetine not only reduces the peak amplitude of Kv4.3 currents but also accelerates the decay rate of current inactivation in a concentration-dependent manner. Dapoxetine decreases the integral of the Kv4.3 currents over the duration of a depolarizing pulse with an IC50 of 5.3 μM. Dapoxetine also causes a substantial acceleration in closed-state inactivation. Dapoxetine produces a significant use-dependent block, which is accompanied by a delayed recovery from inactivation of Kv4.3 currents. [1] Dapoxetine decreases the peak amplitude of Kv1.5 currents and accelerates the decay rate of current inactivation in a concentration-dependent manner with an IC50 of 11.6 μM. Dapoxetine decreases the tail current amplitude and slows the deactivation process of Kv1.5, which results in a tail crossover phenomenon. Dapoxetine produces a use-dependent block of Kv1.5 at frequencies of 1 and 2 Hz and slowed the time course for recovery of inactivation. [2] Dapoxetine also appears to be a useful adjunct to morphine, lowering the threshold for analgesia, although Dapoxetine itself has negligible analgesic activity. Dapoxetine is the D-enantiomer of LY 243917 and is 3.5 times more potent as a serotonin reuptake inhibitor than the L-enantiomer. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 68 mg/mL
(198.9 mM)
Water 68 mg/mL
(198.9 mM)
Ethanol '68 mg/mL

Chemical Information

Molecular Weight 341.87
Formula

C21H23NO.HCl

CAS No. 129938-20-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)C(CCOC1=CC=CC2=CC=CC=C21)C3=CC=CC=C3.Cl

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03018743 Unknown status Drug: Dapoxetine Premature Ejaculation Pusan National University Hospital January 2017 --
NCT01928563 Unknown status Drug: Dapoxetine|Drug: Udenafil|Drug: Udenafil+Dapoxetine Healthy Male Subjects Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd. September 2013 Phase 1
NCT01366664 Completed Drug: Treatment sequence 2|Drug: Treatment sequence 1 Ejaculation Janssen Research & Development LLC April 2011 Phase 1
NCT01063881 Completed Drug: Dapoxetine Sexual Dysfunction Physiological Johnson & Johnson Pte Ltd May 2010 Phase 3
NCT00211094 Completed Drug: Dapoxetine Ejaculation Alza Corporation DE USA Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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