Dapoxetine HCl | Priligy | LY-210448 | CAS#129938-20-1 | CAS#119356-77-3 | Selective Serotonin Reuptake Inhibitor

MedKoo Cat#: 329019 | Name: Dapoxetine HCl

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Description:

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

Dapoxetine HCl, also known as Priligy and LY-210448, is a selective serotonin reuptake inhibitor used to treat premature ejaculation in men.

Chemical Structure

Dapoxetine HCl

CAS#129938-20-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 329019

Name: Dapoxetine HCl

CAS#: 129938-20-1 (HCl)

Chemical Formula: C21H24ClNO

Exact Mass: 0.0000

Molecular Weight: 341.88

Elemental Analysis: C, 73.78; H, 7.08; Cl, 10.37; N, 4.10; O, 4.68

Price and Availability

Size	Price	Availability	Quantity
1g	USD 250.00	2 Weeks
5g	USD 450.00	2 Weeks

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Related CAS #

119356-77-3 (free base) 129938-20-1 (HCl)

Synonym

Dapoxetine HCl; LY-210448; LY 210448; LY210448; Priligy; Dapoxetine Hydrochloride;

IUPAC/Chemical Name

(S)-N,N-dimethyl-3-(naphthalen-1-yloxy)-1-phenylpropan-1-amine hydrochloride

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

SMILES Code

CN(C)[C@@H](CCOC1=C2C=CC=CC2=CC=C1)C3=CC=CC=C3.[H]Cl

Appearance

Solid powder

Purity

>97% (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

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

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

Related CAS# 119356-77-3 (Dapoxetine ) 129938-20-1 (Dapoxetine HCl)

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Dapoxetine (hydrochloride) is an analytical reference standard that is categorized as a selective serotonin reuptake inhibitor and provides improvement in several parameters related to premature ejaculation in clinical trials.

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/

	Solvent	mg/mL	mM
Solubility
	DMSO	16.0	46.80
	Ethanol	25.0	73.13

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 341.88 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.

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:

In vivo protocol:

1: Aziz A, Mohamed TA, Khamees N, Derar AR. Comparative Study of PVC-Free All-Solid-State, PVC Membrane, and Carbon Paste Ion-Selective Electrodes for the Determination of Dapoxetine Hydrochloride in Pharmaceutical Formulation. J AOAC Int. 2016 Sep 1. [Epub ahead of print] PubMed PMID: 27590599. 2: De Hong C, Ren LL, Yu H, Qiang W. The role of dapoxetine hydrochloride on-demand for the treatment of men with premature ejaculation. Sci Rep. 2014 Dec 1;4:7269. doi: 10.1038/srep07269. Review. PubMed PMID: 25434754; PubMed Central PMCID: PMC4248279. 3: Fouad SA, Shamma RN, Basalious EB, El-Nabarawi MA, Tayel SA. Novel instantly-soluble transmucosal matrix (ISTM) using dual mechanism solubilizer for sublingual and nasal delivery of dapoxetine hydrochloride: In-vitro/in-vivo evaluation. Int J Pharm. 2016 May 30;505(1-2):212-22. doi: 10.1016/j.ijpharm.2016.04.006. Epub 2016 Apr 5. PubMed PMID: 27063851. 4: Zhu Y, Liu Z, Li H, Ye D, Zhou W. A novel and practical asymmetric synthesis of dapoxetine hydrochloride. Beilstein J Org Chem. 2015 Dec 17;11:2641-5. doi: 10.3762/bjoc.11.283. eCollection 2015. PubMed PMID: 26734109; PubMed Central PMCID: PMC4685759. 5: Maha H, Amira K, Mohamed A, Ahmed Emad el G. A novel liquid chromatographic method with fluorescence detection for quantitation of tadalafil and dapoxetine hydrochloride in pharmaceutical dosage form and human plasma. Se Pu. 2015 Jul;33(7):765-70. PubMed PMID: 26672207. 6: 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. Review. PubMed PMID: 27456527. 7: Zhang WM, Qiang W, Ying-Fei W, Ming S, Wang R. Development and validation of a sensitive UPLC-MS/MS method for the simultaneous determination of dapoxetine and its two metabolites in human plasma. J Pharm Biomed Anal. 2016 Feb 5;119:45-9. doi: 10.1016/j.jpba.2015.11.018. PubMed PMID: 26641706. 8: Sayed RH, Saad MA, El-Sahar AE. Dapoxetine attenuates testosterone-induced prostatic hyperplasia in rats by the regulation of inflammatory and apoptotic proteins. Toxicol Appl Pharmacol. 2016 Sep 27. pii: S0041-008X(16)30290-3. doi: 10.1016/j.taap.2016.09.024. PubMed PMID: 27687055. 9: Chen XY, Qu YW, Wang SG. [Efficacy and safety of dapoxetine in the treatment of premature ejaculation]. Zhonghua Nan Ke Xue. 2016 May;22(5):411-4. Chinese. PubMed PMID: 27416664. 10: Attia AK, Souaya ER, Soliman EA. Thermal Analysis Investigation of Dapoxetine and Vardenafil Hydrochlorides using Molecular Orbital Calculations. Adv Pharm Bull. 2015 Nov;5(4):523-9. doi: 10.15171/apb.2015.071. Epub 2015 Nov 30. PubMed PMID: 26819925; PubMed Central PMCID: PMC4729354. 11: Simsek A, Kirecci SL, Kucuktopcu O, Ozgor F, Akbulut MF, Sarilar O, Ozkuvanci U, Gurbuz ZG. Comparison of paroxetine and dapoxetine, a novel selective serotonin reuptake inhibitor in the treatment of premature ejaculation. Asian J Androl. 2014 Sep-Oct;16(5):725-7. doi: 10.4103/1008-682X.128467. PubMed PMID: 24830690; PubMed Central PMCID: PMC4215669. 12: Li RF, Fu JM, Lv XZ, Zhang DT, Pan YY, Rao DP, Yu KY. Effects of Evodiamine on the Pharmacokinetics of Dapoxetine and Its Metabolite Desmethyl Dapoxetine in Rats. Pharmacology. 2016;97(1-2):43-7. doi: 10.1159/000441568. Epub 2015 Nov 21. PubMed PMID: 26588583. 13: Mirone V, Arcaniolo D, Rivas D, Bull S, Aquilina JW, Verze P; PAUSE study team. Results from a prospective observational study of men with premature ejaculation treated with dapoxetine or alternative care: the PAUSE study. Eur Urol. 2014 Apr;65(4):733-9. doi: 10.1016/j.eururo.2013.08.018. Epub 2013 Aug 22. PubMed PMID: 23993257. 14: Hsueh TY, Ho JK, Lin LC, Chiu AW, Lin CH, Tsai TH. Herb-drug interaction of Epimedium extract on the pharmacokinetic of dapoxetine in rats. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Mar 1;1014:64-9. doi: 10.1016/j.jchromb.2016.02.001. Epub 2016 Feb 4. PubMed PMID: 26874879. 15: Abdlekawy KS, Donia AM, Elbarbry F. Effects of Grapefruit and Pomegranate Juices on the Pharmacokinetic Properties of Dapoxetine and Midazolam in Healthy Subjects. Eur J Drug Metab Pharmacokinet. 2016 Jun 13. [Epub ahead of print] PubMed PMID: 27294349.