Dapoxetine Free Base

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 413462

CAS#: 119356-77-3 (free base)

Description: Dapoxetine Free Base, marketed as Priligy, among others, is a medication used for the treatment of premature ejaculation in men 18–64 years old. Dapoxetine works by inhibiting the serotonin transporter, increasing serotonin's action at the postsynaptic cleft, and as a consequence promoting ejaculatory delay.

Chemical Structure

img
Dapoxetine Free Base
CAS# 119356-77-3 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 413462
Name: Dapoxetine Free Base
CAS#: 119356-77-3 (free base)
Chemical Formula: C21H23NO
Exact Mass: 305.18
Molecular Weight: 305.420
Elemental Analysis: C, 82.58; H, 7.59; N, 4.59; O, 5.24

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 119356-77-3 (free base)   129938-20-1 (HCl)  

Synonym: Dapoxetine Free Base; LY210448; LY-210448; LY 210448

IUPAC/Chemical Name: Benzenemethanamine, N,N-dimethyl-alpha-(2-(1-naphthalenyloxy)ethyl)-, (+)-

InChi Key: USRHYDPUVLEVMC-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H23NO/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

SMILES Code: CN(C)C(CCOC1=C2C=CC=CC2=CC=C1)C3=CC=CC=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: to be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Dapoxetine is a selective serotonin reuptake inhibitor, for the treatment of premature ejaculation.
In vitro activity: The purpose of this study was to investigate the therapeutic efficacy of transdermal delivery of DH (Dapoxetine HCl) in transethosome nanovesicles (TENVs). The TENV formulations were assessed for entrapment efficiency (EE-%), vesicle size, zeta potential, in vitro DH release, and skin permeation. The release behavior of DH from DH-TENVs was investigated to confirm whether the DH-TENVs had the ability to release DH in a sustained manner. Rapid DH release from free DH solution in the dialysis bag was observed, with approximately 95% of the DH being released in the first 3 h (Figure S1A–C). In contrast, the DH in DH-TENVs demonstrated a slow and controlled release, with about 53–85% of the DH being released within 8 h (Table 2). The results indicate that DH-TENVs can improve transdermal delivery of DH and thereby alleviate RA. Reference: Int J Nanomedicine. 2020; 15: 1517–1535. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7065716/
In vivo activity: The effects of 8-OH-DPAT and dapoxetine on the sexual behavior of male rats were investigated in this study. Dapoxetine significantly reduced the ejaculation performance at a dose of 60 mg/kg by delaying the latency of mounts and decreasing the latency of ejaculation and post-ejaculatory interval. Significant differences in the gene expression profiles were observed in the EJ (257 genes), DPAT (349 genes) and the DAP (207 genes) compared with the control rats In the present study, Drd4 was significantly upregulated (fold change: 2.42) following dapoxetine treatment whereas no such trend was noted regarding other 5-HT receptor or transporter genes. Reference: Acta Pharm Sin B. 2017 May; 7(3): 381–389. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5430880/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 0.0 0.00

Preparing Stock Solutions

The following data is based on the product molecular weight 305.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Aldawsari HM, Badr-Eldin SM. Enhanced pharmacokinetic performance of dapoxetine hydrochloride via the formulation of instantly-dissolving buccal films with acidic pH modifier and hydrophilic cyclodextrin: Factorial analysis, in vitro and in vivo assessment. J Adv Res. 2020 May 1;24:281-290. doi: 10.1016/j.jare.2020.04.019. PMID: 32419956; PMCID: PMC7215178. 2. Salem HF, Nafady MM, Kharshoum RM, Abd El-Ghafar OA, Farouk HO. Mitigation of Rheumatic Arthritis in a Rat Model via Transdermal Delivery of Dapoxetine HCl Amalgamated as a Nanoplatform: In vitro and in vivo Assessment. Int J Nanomedicine. 2020 Mar 6;15:1517-1535. doi: 10.2147/IJN.S238709. PMID: 32189966; PMCID: PMC7065716. 3. Qin X, Ma X, Tu D, Luo Z, Huang J, Mo C. The effect of 8-OH-DPAT and dapoxetine on gene expression in the brain of male rats during ejaculation. Acta Pharm Sin B. 2017 May;7(3):381-389. doi: 10.1016/j.apsb.2016.11.004. Epub 2017 Mar 14. PMID: 28540176; PMCID: PMC5430880.
In vitro protocol: 1. Aldawsari HM, Badr-Eldin SM. Enhanced pharmacokinetic performance of dapoxetine hydrochloride via the formulation of instantly-dissolving buccal films with acidic pH modifier and hydrophilic cyclodextrin: Factorial analysis, in vitro and in vivo assessment. J Adv Res. 2020 May 1;24:281-290. doi: 10.1016/j.jare.2020.04.019. PMID: 32419956; PMCID: PMC7215178. 2. Salem HF, Nafady MM, Kharshoum RM, Abd El-Ghafar OA, Farouk HO. Mitigation of Rheumatic Arthritis in a Rat Model via Transdermal Delivery of Dapoxetine HCl Amalgamated as a Nanoplatform: In vitro and in vivo Assessment. Int J Nanomedicine. 2020 Mar 6;15:1517-1535. doi: 10.2147/IJN.S238709. PMID: 32189966; PMCID: PMC7065716.
In vivo protocol: 1. Aldawsari HM, Badr-Eldin SM. Enhanced pharmacokinetic performance of dapoxetine hydrochloride via the formulation of instantly-dissolving buccal films with acidic pH modifier and hydrophilic cyclodextrin: Factorial analysis, in vitro and in vivo assessment. J Adv Res. 2020 May 1;24:281-290. doi: 10.1016/j.jare.2020.04.019. PMID: 32419956; PMCID: PMC7215178. 2. Qin X, Ma X, Tu D, Luo Z, Huang J, Mo C. The effect of 8-OH-DPAT and dapoxetine on gene expression in the brain of male rats during ejaculation. Acta Pharm Sin B. 2017 May;7(3):381-389. doi: 10.1016/j.apsb.2016.11.004. Epub 2017 Mar 14. PMID: 28540176; PMCID: PMC5430880

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Li J, Liu D, Wu J, Fan X, Dong Q. Dapoxetine for the treatment of premature ejaculation: a meta-analysis of randomized controlled trials with trial sequential analysis. Ann Saudi Med. 2018 Sep-Oct;38(5):366-375. doi: 10.5144/0256-4947.2018.366. PMID: 30284992; PMCID: PMC6180218.

2: Dapoxetine: LY 210448. Drugs R D. 2005;6(5):307-11. doi: 10.2165/00126839-200506050-00007. PMID: 16128601.

3: Zhao GJ, Guo Q, Li YF, Zhang YG. Efficacy and safety of dapoxetine for premature ejaculation: an updated systematic review and meta-analysis. Sex Health. 2019 Aug;16(4):301-313. doi: 10.1071/SH18005. PMID: 32172793.

4: McMahon CG. Dapoxetine for premature ejaculation. Expert Opin Pharmacother. 2010 Jul;11(10):1741-52. doi: 10.1517/14656566.2010.493174. PMID: 20540653.

5: Sangkum P, Badr R, Serefoglu EC, Hellstrom WJ. Dapoxetine and the treatment of premature ejaculation. Transl Androl Urol. 2013 Dec;2(4):301-11. doi: 10.3978/j.issn.2223-4683.2013.12.01. PMID: 26816743; PMCID: PMC4708110.

6: Hoy SM, Scott LJ. Dapoxetine: in premature ejaculation. Drugs. 2010 Jul 30;70(11):1433-43. doi: 10.2165/11204750-000000000-00000. PMID: 20614950.

7: Abu El-Hamd M, Abdelhamed A. Comparison of the clinical efficacy and safety of the on-demand use of paroxetine, dapoxetine, sildenafil and combined dapoxetine with sildenafil in treatment of patients with premature ejaculation: A randomised placebo-controlled clinical trial. Andrologia. 2018 Feb;50(1). doi: 10.1111/and.12829. Epub 2017 May 12. PMID: 28497478.

8: Wang YB, Mao Y, Wei Q, Wu TX, Dong Q. [Dapoxetine in treatment of premature ejaculation: a systematic review]. Beijing Da Xue Xue Bao Yi Xue Ban. 2010 Aug 18;42(4):425-32. Chinese. PMID: 20721257.

9: Dapoxetine for premature ejaculation. Drug Ther Bull. 2014 Mar;52(3):30-3. doi: 10.1136/dtb.2014.3.0240. PMID: 24627135.

10: Russo A, Capogrosso P, Ventimiglia E, La Croce G, Boeri L, Montorsi F, Salonia A. Efficacy and safety of dapoxetine in treatment of premature ejaculation: an evidence-based review. Int J Clin Pract. 2016 Sep;70(9):723-33. doi: 10.1111/ijcp.12843. Epub 2016 Jul 25. PMID: 27456527.