Dapoxetine HCl powder CAS 119356-77-3, high purity raw material for male health research

Dapoxetine Hydrochloride CAS 129938-20-1 99% Powder LY-210448 Selective Short-Acting SSRI Inhibitor API for Sexual Dysfunction Research

99% Dapoxetine Hydrochloride powder CAS 129938-20-1, also known as LY-210448 hydrochloride, is a potent, short-acting selective serotonin reuptake inhibitor (SSRI) with unique pharmacological characteristics. Compared with conventional long-acting SSRIs, Dapoxetine hydrochloride features rapid absorption, fast metabolic clearance and short half-life, specifically targeting serotonin transporter (SERT) to block serotonin reuptake and increase synaptic serotonin concentration. It effectively regulates neural excitability, serves as a classic pharmaceutical API raw material for male sexual dysfunction research, and also acts as a Kv4.3 potassium channel blocker for neurological pharmacological studies. Widely applied in pharmaceutical intermediate synthesis, neuropharmacology mechanism research, SSRI drug activity verification and new drug formulation development.
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Dapoxetine Hydrochloride (CAS 129938-20-1) SSRI | Potent SERT Inhibitor (IC50 1.12 nM), Premature-Ejaculation & Serotonin-Transporter Research Compound

Dapoxetine Hydrochloride CAS 129938-20-1
Selective Serotonin Reuptake Inhibitor (SSRI) for Premature-Ejaculation Research

Dapoxetine hydrochloride (CAS 129938-20-1), the active ingredient of Priligy, is a short-acting, potent and selective serotonin reuptake inhibitor (SSRI) with a serotonin-transporter (SERT/SLC6A4) IC50 of ~1.12 nM. By blocking 5-HT reuptake it raises the ejaculatory threshold. Molecular formula C21H23NO·HCl, MW 341.87. Research-grade with COA.

SSRI SERT Serotonin Transporter Premature Ejaculation Priligy SLC6A4 PE Research On-Demand
Request a Quote Technical Specs
341.87
MW (C21H23NO·HCl)
1.12 nM
SERT IC50
SSRI
Selective vs NET/DAT weak

Molecular Information

Name: Dapoxetine Hydrochloride
CAS: 129938-20-1
Formula: C21H23NO·HCl
MW: 341.87 g/mol
Class: Phenylpropylamine SSRI
Core: (S)-N,N-dimethyl-3-(naphthalen-1-yloxy)-1-phenylpropan-1-amine HCl
Target: SERT (SLC6A4)
IC50: ~1.12 nM
MP: 180-182 C
Appearance: White to off-white powder
Synonyms: Priligy / LY-210448
Storage: RT desiccated / -20 C
🧪
CAS Number
129938-20-1
⚖️
Molecular Weight
341.87
🎯
Primary Activity
SSRI (SERT)
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for Dapoxetine Hydrochloride (CAS 129938-20-1)

📋 Physicochemical Properties

  • Product NameDapoxetine Hydrochloride
  • IUPAC Core(1S)-N,N-dimethyl-3-(naphthalen-1-yloxy)-1-phenylpropan-1-amine hydrochloride
  • CAS Number129938-20-1
  • SynonymsPriligy; LY-210448
  • Molecular FormulaC21H23NO·HCl
  • Molecular Weight341.87 g/mol
  • SourceSynthetic small molecule (Eli Lilly, ex LY-210448)
  • AppearanceWhite to off-white powder
  • Melting Point180-182 C
  • Water Solubility~68 mg/mL
  • Organic SolubilityDMSO >=20 mg/mL; methanol; ethanol
  • Compound ClassPhenylpropylamine / SSRI
  • HS Code2934.99

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormCrystalline powder
  • Primary TargetSerotonin transporter (SERT / SLC6A4)
  • Pathway ReadoutElevated synaptic 5-HT; [3H]5-HT uptake inhibition
  • SelectivitySelective SERT; weak NET/DAT; blocks Kv4.3 / Kv1.5 K+ channels
  • Storage ConditionRoom temp desiccated / -20 C, sealed, protect from light
  • Solution StabilityAliquot DMSO stocks; avoid freeze-thaw
  • ShippingRoom temp / blue ice recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1KG / 5KG / 10KG / 25KG / 1TON
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Pathway Nodes

Dapoxetine's functional reach is the central serotonergic system; its primary molecular target is the serotonin transporter SLC6A4, with secondary modulation of voltage-gated potassium channels.

🧬 SERT (SLC6A4) 🔄 Serotonin (5-HT) Reuptake 🔗 5-HT1A / 1B / 2C Receptors 🧠 Lateral Paragigantocellular Nucleus ⚡ Ejaculatory Reflex Pathway 🔌 Voltage-Gated K+ Channels (Kv4.3) 🧪 Presynaptic 5-HT Clearance 📈 Postsynaptic 5-HT Signaling 🧠 Raphe Nuclei 🧩 Hypothalamus 🍆 Penile Smooth Muscle (indirect) 🛡️ Cytokine Modulation (indirect)

How Dapoxetine Works: Blocking SERT to Delay the Ejaculatory Reflex

Dapoxetine stops the serotonin transporter from clearing 5-HT, raising synaptic serotonin and raising the ejaculatory threshold

1

Sexual Stimulus Activates the Ejaculatory Circuit

Ejaculation is coordinated by a spinal reflex modulated by supraspinal centers (the lateral paragigantocellular nucleus) and serotonin (5-HT) pathways originating in the raphe nuclei. Under baseline conditions the serotonin transporter (SERT/SLC6A4) rapidly clears synaptic 5-HT, limiting serotonergic tone on the reflex pathway.

2

SERT Inhibition Raises Synaptic Serotonin

Dapoxetine binds SERT with ~1.12 nM potency, blocking reuptake of 5-HT into the presynaptic neuron. Extracellular serotonin accumulates and engages inhibitory 5-HT receptors (notably 5-HT1B/1A/2C) on the ejaculatory reflex pathway, raising the threshold for emission and expulsion and prolonging intravaginal ejaculatory latency time (IELT).

3

Ejaculatory Delay & Rapid Kinetics

Because dapoxetine is absorbed and eliminated quickly (Tmax ~1-1.3 h, t1/2 ~1.5 h), it is taken on-demand 1-3 h before activity — unlike daily SSRIs. This fast on/off profile is precisely why it was developed for premature ejaculation rather than as an antidepressant.

⚖️ Dapoxetine vs Paroxetine vs Other SSRIs

  • Dapoxetine (this product)SERT IC50 ~1.12 nM; on-demand, Tmax ~1 h, t1/2 ~1.5 h
  • ParoxetineSSRI, longer t1/2 (~21 h); used off-label for PE
  • Sertraline / FluoxetineDaily SSRIs with slower onset, used off-label for PE
  • Shared MechanismAll block SERT; dapoxetine is fast-acting & short-lived
  • Key DistinctionOn-demand PK enables event-driven dosing
  • Off-targetDapoxetine also blocks Kv4.3 / Kv1.5 potassium channels

♻️ Downstream Biological Consequences

  • Second MessengerElevated synaptic 5-HT
  • Receptors5-HT1B / 1A / 2C engagement
  • ReflexIncreased ejaculatory threshold / longer IELT
  • BrainIncreased serotonergic tone in lPAG
  • ChannelsKv4.3 / Kv1.5 potassium-channel block
  • BehaviorDelayed ejaculation, event-driven

Research Applications & Models

From the first on-demand premature-ejaculation therapy to a clean serotonergic probe, dapoxetine spans clinical and basic neuroscience research.

⏱️

Premature Ejaculation Models

The reference on-demand SSRI for PE; used to extend intravaginal ejaculatory latency time (IELT) in rodent and clinical models and as the comparator for new PE agents.

SERT / 5-HT
🧠

Serotonin Transporter (SERT) Research

A fiducial SERT/SLC6A4 ligand for radioligand-binding, [3H]5-HT uptake and electrophysiology assays probing serotonergic neurotransmission.

SLC6A4
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K+ Channel Pharmacology

Studied for block of voltage-gated potassium channels (Kv4.3, Kv1.5), relevant to cardiac and neuronal excitability research.

Kv channels
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Ejaculatory Reflex Circuit

Used to map the lPAG / spinal ejaculatory generator and the 5-HT receptor subtypes controlling emission and expulsion.

lPAG / Spinal
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PK / On-Demand Dosing Studies

A model for rapid-absorption, short-half-life CNS drug kinetics and event-driven dosing design.

Rapid PK
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SSRI Class Profiling

Benchmarked against paroxetine/sertraline to separate SERT blockade from downstream behavioral and autonomic effects.

SSRI panel

Key Literature & Landmark Publications

The pharmacology and clinical validation of dapoxetine in premature-ejaculation research.

McMahon CG. Dapoxetine: a new option in the medical management of premature ejaculation. Ther Adv Urol. 2012;4(5):233-51.
doi: 10.1177/1756287212452857
Hellstrom WJ, et al. Update on treatments for premature ejaculation. Int J Clin Pract. 2011;65(1):16-26.
doi: 10.1111/j.1742-1241.2010.02456.x
Clément P, et al. Supraspinal site of action for the inhibition of ejaculatory reflex by dapoxetine. Eur Urol. 2007;51(3):825-32.
doi: 10.1016/j.eururo.2006.07.026
Jeong I, et al. Block of cloned Kv4.3 potassium channels by dapoxetine. Neuropharmacology. 2012;62(7):2261-6.
doi: 10.1016/j.neuropharm.2012.01.010
Kendirci M, et al. Dapoxetine, a novel selective serotonin transport inhibitor for the treatment of premature ejaculation. Ther Clin Risk Manag. 2007;3(2):277-89.
Landmark reference

Available Sizes & Ordering

Research-grade Dapoxetine Hydrochloride (CAS 129938-20-1) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard1KGIn StockSERT / 5-HT uptake & PE modelsSame/next-day ship
Medium5KGIn StockNeurotransmitter & behavioral studiesSame/next-day ship
Large10KGIn StockLong-term in vivo & formulation studiesSame/next-day ship
Bulk25KGIn StockFormulation, coating and process developmentQuote to confirm
Industrial1TONMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is dapoxetine and what does it do?
Dapoxetine hydrochloride (CAS 129938-20-1) is a selective serotonin reuptake inhibitor (SSRI) and the active ingredient of Priligy, developed specifically for premature ejaculation. It blocks the serotonin transporter SERT (SLC6A4) with an IC50 of ~1.12 nM, raising synaptic 5-HT and the ejaculatory threshold. Formula C21H23NO·HCl, MW 341.87, SERT IC50 ~1.12 nM.
How is dapoxetine different from other SSRIs like paroxetine?
All three block SERT, but dapoxetine is fast-acting and short-lived (Tmax ~1 h, t1/2 ~1.5 h), enabling on-demand, event-driven dosing 1-3 h before activity. Paroxetine and sertraline have long half-lives and are used off-label as daily SSRIs. Dapoxetine also blocks Kv4.3 / Kv1.5 potassium channels, a property shared by few SSRIs.
What is the mechanism in premature ejaculation?
Sexual stimuli activate a spinal ejaculatory reflex gated by serotonergic (5-HT) pathways from the raphe nuclei. Dapoxetine blocks SERT, so 5-HT accumulates in the synapse and engages inhibitory 5-HT1B/1A/2C receptors on the reflex pathway, raising the threshold for emission and expulsion and prolonging IELT. Like other SSRIs, it depends on the presence of serotonergic tone.
What are the key experimental readouts?
The canonical readouts are [3H]5-HT uptake inhibition in SERT-expressing cells, radioligand-binding affinity at SLC6A4, synaptic 5-HT elevation, and behavioral IELT in validated PE models. Off-target potassium-channel block is measured by patch-clamp on Kv4.3 / Kv1.5.
How soluble is dapoxetine and how should it be prepared?
Dapoxetine HCl is soluble in DMSO (>=20 mg/mL) and notably in water (~68 mg/mL). For cell assays typical working concentrations are low nanomolar to low micromolar; dilute DMSO stock into pre-warmed medium keeping final DMSO <=0.1% v/v. Store the solid desiccated at room temperature or -20 C, protected from light; aliquot stocks to avoid freeze-thaw.
Is QC documentation provided? Can I request a sample?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, NMR structural confirmation and MS data. MSDS/SDS, residual-solvent data and Certificates of Origin are available on request. Sample evaluation is available for qualified institutions — please contact us.

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Research-grade Dapoxetine Hydrochloride (CAS 129938-20-1) — purity ≥98% HPLC, COA included
The on-demand, fast-acting SERT/SLC6A4 inhibitor for premature-ejaculation and serotonergic signaling research — request a quote today

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