Dapoxetine HCl (LY-210448 HCl)

Alias: LY-210448; Dapoxetine HCl; LY 210448; LY210448; Priligy
Cat No.:V0977 Purity: ≥98%
Dapoxetine HCl (formerly known as LY210448; LY-210448; trade name Priligy), an antidepressant, is a novel, potent, short-acting and selective serotonin reuptake inhibitor (SSRI) that has alto been used for the treatment of premature ejaculation.
Dapoxetine HCl (LY-210448 HCl) Chemical Structure CAS No.: 129938-20-1
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
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1g
2g
5g
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Other Forms of Dapoxetine HCl (LY-210448 HCl):

  • Dapoxetine
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Dapoxetine HCl (formerly known as LY210448; LY-210448; trade name Priligy), an antidepressant, is a novel, potent, short-acting and selective serotonin reuptake inhibitor (SSRI) that has alto been used for the treatment of premature ejaculation. It is a novel, short-acting selective serotonin reuptake inhibitor that is marketed to treat men's premature ejaculation. Granisetron inhibits feline isolated ventricular myocytes' delayed rectifier current (IK) at a 4.3 mM KD. Granisetron exhibits an inherent voltage dependence when the depolarization increases the block.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT
ln Vitro

In vitro activity: Dapoxetine hydrochloride binds to transporters of dopamine, norepinephrine, and 5-HT. It then inhibits the uptake of dopamine, norepinephrine, and 5-HT in the following potent order: 55-HT >norepinephrine≫dopamine. Dapoxetine hydrochloride blocks the uptake of [3H]5-HT by the 5-HT reuptake transporter at a concentration of 1.12 nM. Dapoxetine also blocks the uptake of [3H]dopamine by the dopamine reuptake transporter and [3H]norepinephrine into cells using the norepinephrine reuptake transporter, with IC50 values of 202 nM and 1720 nM, respectively.[1]

ln Vivo
Dapoxetine hydrochloride (oral gavage; 1-10 mg/kg; once daily) significantly reduces the weight gain and relative weight gain of the prostate caused by testosterone and attenuates the prostatic hyperplasia caused by testosterone in rats[2].
Animal Protocol
Adult male Wistar rats
1 mg/kg, 5 mg/kg, 10 mg/kg
Oral gavage; 1-10 mg/kg; once daily
References

[1]. Dapoxetine, a novel selective serotonin transport inhibitor for the treatment of premature ejaculation. Ther Clin Risk Manag. 2007 Jun;3(2):277-89.

[2]. Dapoxetine attenuates testosterone-induced prostatic hyperplasia in rats by the regulation of inflammatory and apoptotic proteins. Toxicol Appl Pharmacol. 2016 Nov 15;311:52-60.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H24CLNO
Molecular Weight
341.87
Exact Mass
341.15
Elemental Analysis
C, 73.78; H, 7.08; Cl, 10.37; N, 4.10; O, 4.68
CAS #
129938-20-1
Related CAS #
Dapoxetine-d7 hydrochloride; Dapoxetine; 119356-77-3; (rac)-Dapoxetine-d6 hydrochloride
Appearance
Solid powder
SMILES
CN(C)[C@@H](CCOC1=CC=CC2=CC=CC=C21)C3=CC=CC=C3.Cl
InChi Key
IHWDIQRWYNMKFM-BDQAORGHSA-N
InChi Code
InChI=1S/C21H23NO.ClH/c1-22(2)20(18-10-4-3-5-11-18)15-16-23-21-14-8-12-17-9-6-7-13-19(17)21;/h3-14,20H,15-16H2,1-2H3;1H/t20-;/m0./s1
Chemical Name
(1S)-N,N-dimethyl-3-naphthalen-1-yloxy-1-phenylpropan-1-amine;hydrochloride
Synonyms
LY-210448; Dapoxetine HCl; LY 210448; LY210448; Priligy
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: ~68 mg/mL (~198.9 mM)
Water: <1 mg/mL
Ethanol: ~68 mg/mL (~198.9 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9251 mL 14.6254 mL 29.2509 mL
5 mM 0.5850 mL 2.9251 mL 5.8502 mL
10 mM 0.2925 mL 1.4625 mL 2.9251 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00211094 Completed Drug: Dapoxetine Ejaculation Alza Corporation, DE, USA June 2004 Phase 3
NCT01419470 Completed Drug: dapoxetine Premature Ejaculation Yuhan Corporation February 2011 Phase 1
Phase 2
NCT01366664 Completed Drug: Treatment sequence 2
Drug: Treatment sequence 1
Ejaculation Janssen Research &
Development, LLC
April 2011 Phase 1
NCT01063855 Completed Drug: Dapoxetine
Drug: Placebo
Erectile Dysfunction
Sexual Dysfunction
Johnson & Johnson Pharmaceutical
Research & Development, L.L.C.
April 2010 Phase 3
NCT01230762 Completed Drug: dapoxetine Ejaculation Alza Corporation, DE, USA April 2005 Phase 3
Biological Data
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