Name: Dapoxetine HCl
Brand: Selleck Chemicals
SKU: S1869
Availability: InStock
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other 5-HT Receptor Inhibitors	WAY-100635 Maleate Puerarin Serotonin (5-HT) HCl SB269970 HCl Ketanserin BRL-15572 Dihydrochloride Nuciferine RS-127445 Flopropione Azacyclonol

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (198.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 68 mg/mL

Ethanol : 68 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
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.

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

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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.

Chemical Information, Storage & Stability

Molecular Weight	341.87	Formula	C₂₁H₂₃NO.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	129938-20-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY-210448			Smiles	CN(C)C(CCOC1=CC=CC2=CC=CC=C21)C3=CC=CC=C3.Cl

Mechanism of Action

Targets/IC₅₀/Ki	5-HT
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. 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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22192593/ [2] https://pubmed.ncbi.nlm.nih.gov/22538641/ [3] https://pubmed.ncbi.nlm.nih.gov/16128601/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Dapoxetine HCl 5-HT Receptor inhibitor

Chemical Structure

Molecular Weight: 341.87