Nutrabiotech Icariin 99% 1G Powder, 99% high purity icariin powder, Epimedium brevicornu extract, neuroprotective botanical raw material, anti-aging and vitality support powder

Icariin CAS 56692‑02‑5 98% High‑Purity Flavonoid Glycoside Epimedium Extract PDE5 Inhibitor

High‑purity 98% Icariin crystalline powder CAS 56692‑02‑5, natural Epimedium‑origin flavonoid glycoside with osteogenic, anti‑inflammatory and neuroprotective activities for life‑science pharmacological research.
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Icariin (CAS 56692-02-5) Natural PDE5 Inhibitor | Osteogenesis, Phytoestrogen, Bone Health

Icariin CAS 56692-02-5
Natural PDE5 Inhibitor & Osteogenic Flavonoid

A prenylated flavonol glycoside isolated from Epimedium (Horny Goat Weed). Icariin is a potent natural PDE5 inhibitor (IC50 0.43 μM), a phytoestrogen, a PPARα activator, and a stimulator of the Wnt/β-catenin and BMP pathways that drive osteoblast differentiation. ~91.2% is converted by gut bacteria to the active metabolite icariside II — conferring prodrug-like pharmacokinetics. Validated for bone density preservation in a 24-month randomized clinical trial.

PDE5 Inhibitor Phytoestrogen PPARα Activator Bone Health Wnt/β-catenin Neuroprotective Osteoblast Differentiation
Request a Quote Technical Specs
676.66
MW (C33H40O15)
0.43 μM
PDE5 IC50
≥98%
Purity (HPLC)

Molecular Information

Name: Icariin
CAS: 56692-02-5
Formula: C33H40O15
MW: 676.66 g/mol
SMILES: COc1ccc(cc1)-c1oc2c(
  CC=C(C)C)c(OC3OC...)
InChIKey: TZJALUIVHRYQQB
  -XLRXWWTNSA-N
Appearance: Yellow to light brown powder
Synonyms: Ieariline / Epimedin
  extract / Horny Goat Weed flavonoid
Source: Epimedium species
Storage: 2-8°C, protected from light
🧪
CAS Number
56692-02-5
⚖️
Molecular Weight
676.66
🎯
Primary Activity
PDE5 Inhibitor
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for Icariin (CAS 56692-02-5)

📋 Physicochemical Properties

  • Product NameIcariin
  • IUPAC NameKaempferol 3,7-O-diglycoside 8-prenyl derivative
  • CAS Number56692-02-5
  • SynonymsIeariline / Epimedin extract
  • Molecular FormulaC33H40O15
  • Molecular Weight676.66 g/mol
  • SMILESCOc1ccc(cc1)-c1oc2c(CC=C(C)C)c(OC3OC...)c3ccc(O)cc3-1
  • InChIKeyTZJALUIVHRYQQB-XLRXWWTNSA-N
  • Plant SourceEpimedium brevicornum / sagittatum / koreanum
  • AppearanceYellow to light brown powder
  • HS Code2938.90
  • PubChem CID5318995

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormFine powder
  • ColorYellow to light brown
  • Storage Condition2-8°C, protect from light
  • SolubilityDMSO, ethanol; poorly soluble in water
  • Active MetaboliteIcariside II (91.2% by gut bacteria)
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Signaling Pathways

Icariin's flavonoid skeleton engages a network of receptors and transcription factors central to bone, vascular, metabolic and neuroprotective biology

🧬 PDE5 (IC50 0.43 μM) 🔥 PPARα 🦴 Wnt/β-catenin 🧫 BMP2 ⚡ Runx2 🛡️ Nrf2 ♀️ ERα / ERβ 🩸 eNOS / NO-cGMP 🧠 Neuroinflammation 💪 Osteoblast

How Icariin Works: From PDE5 Blockade to Osteogenesis

Icariin exerts its effects through three coordinated biochemical mechanisms spanning vascular, metabolic and skeletal signaling

1

PDE5 Inhibition & cGMP Elevation

Icariin inhibits phosphodiesterase-5 (IC50 0.43 μM), preventing the breakdown of cyclic GMP. Elevated cGMP through the NO-cGMP pathway promotes vascular smooth-muscle relaxation and underpins its natural PDE5 / erectile-function activity.

2

Phytoestrogenic & PPARα Activation

As a phytoestrogen, icariin binds estrogen receptors (ERα/ERβ), while also activating PPARα to modulate lipid metabolism and energy homeostasis. This dual nuclear-receptor engagement drives its metabolic and cardiometabolic effects.

3

Wnt/β-catenin Osteogenesis & Prodrug Conversion

Icariin activates the Wnt/β-catenin and BMP pathways, upregulating Runx2 to drive osteoblast differentiation and bone formation. Gut bacteria convert ~91.2% of icariin to the more active metabolite icariside II, giving prodrug-like pharmacokinetics.

Research Applications & Disease Models

Icariin's polypharmacology spans bone, sexual, neuro, cardiovascular, metabolic and oncology research

🦴

Bone Health & Osteoporosis

A 24-month RCT in late postmenopausal women showed Epimedium flavonoids preserved femoral neck BMD (+1.6% vs -1.8% placebo) and lumbar spine BMD (+1.3% vs -2.4% placebo). Mechanistic basis: Wnt/β-catenin and BMP2/Runx2-driven osteoblast differentiation.

24-Month RCT
💊

Erectile Dysfunction / PDE5

A natural PDE5 inhibitor (IC50 0.43 μM) that enhances the NO-cGMP pathway, improving corpus cavernosum smooth-muscle relaxation. Investigated as a botanical lead structurally distinct from synthetic PDE5 drugs.

Natural PDE5
🧠

Neuroprotection

Activates the Nrf2 antioxidant pathway and suppresses neuroinflammation, with relevance to Alzheimer's, Parkinson's and ischemic brain injury models. Also modulates cholinergic and neurotrophic signaling.

Nrf2 Activation
❤️

Cardiovascular

Promotes vascular relaxation and improves endothelial function via eNOS/NO-cGMP signaling. Studied for atheroprotection, myocardial protection, and modulation of vascular smooth-muscle proliferation.

Endothelial
🧓

Anti-aging

Delays cellular senescence and modulates stem-cell function and proliferation. Investigated for healthy-aging, tissue regeneration, and protection against age-related functional decline.

Senescence Delay
⚡

Metabolic Health

Activates PPARα to influence lipid metabolism and energy expenditure. Explored for dyslipidemia, fatty liver, and metabolic-syndrome related phenotypes in preclinical models.

PPARα
🧬

Cancer Research

Demonstrates anti-proliferative effects and induction of apoptosis across multiple tumor cell lines. Studied for chemopreventive and adjuvant activities via cell-cycle arrest and pro-apoptotic signaling.

Anti-proliferative
🏃

Exercise Performance

Supports muscle function and fatigue resistance, with studies in endurance and skeletal-muscle regeneration models. Relevant to sports-nutrition and sarcopenia research.

Fatigue Resistance
🌿

Botanical & Natural Product Chemistry

A flagship prenylated flavonol glycoside for studying structure-activity relationships of Epimedium constituents, glycosylation effects, and prodrug conversion to icariside II / icaritin.

Natural Product

Key Literature & Landmark Publications

Seminal papers on icariin's bone, PDE5, and translational pharmacology

Zhang G, Qin L, Shi Y. Epimedium-derived phytoestrogen flavonoids exert beneficial effect on preventing bone loss in late postmenopausal women: a 24-month randomized, double-blind and placebo-controlled trial. Journal of Bone and Mineral Research. 2007;22(7):1072-1079.
doi: 10.1359/jbmr.070405
Dell'Agli M, Galli GV, Cervo S, et al. Potent inhibition of human phosphodiesterase-5 by icariin derivatives. Journal of Natural Products. 2008;71(9):1513-1517.
doi: 10.1021/np800049y
Li H, Xin H, Zhang C, et al. Deciphering the myth of icariin and synthetic derivatives in improving erectile function. Translational Andrology and Urology. 2022;11(1):146-159.
doi: 10.21037/tau-22-4

Available Sizes & Ordering

Research-grade Icariin (CAS 56692-02-5) with full QC documentation; research packs and bulk custom quantities supported

TierPack SizeStock StatusSuitable ForLead Time
Standard1 gIn StockBiochemical / cell-based assaysSame/next-day ship
Medium5 gIn StockIn vivo pharmacology, long-term studiesSame/next-day ship
Large10 gIn StockMulti-lab collaborations, HTSSame/next-day ship
Bulk100 gIn StockProcess development, scale-upQuote to confirm
Industrial1 KGMade 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 Icariin (CAS 56692-02-5), and what makes it unique?
Icariin is a prenylated flavonol glycoside isolated from Epimedium species (Horny Goat Weed), with molecular formula C33H40O15 and MW 676.66. It is unusual among natural products in combining potent PDE5 inhibition (IC50 0.43 μM) with phytoestrogenic, PPARα-activating, and osteogenic activities. It simultaneously engages vascular, metabolic, skeletal and neuroprotective pathways, making it a versatile botanical research tool and a lead for structure-activity optimization.
How does Icariin compare to sildenafil as a PDE5 inhibitor?
Both compounds inhibit phosphodiesterase-5, but differently. Icariin is a naturally derived flavonoid with IC50 ~0.43 μM against PDE5 and broad polypharmacology (ER, PPARα, Wnt/β-catenin). Sildenafil is a synthetic, highly selective PDE5 inhibitor approved for erectile dysfunction. Icariin has lower selectivity and poorer oral bioavailability, so it is used primarily as a research/lead compound rather than a finished therapeutic.
Why is Icariin's bioavailability considered a problem, and what is icariside II?
Icariin has poor water solubility and limited systemic exposure after oral dosing. Gut microbiota metabolize approximately 91.2% of icariin to icariside II (and further to icaritin), which are more readily absorbed and are considered the principal active metabolites responsible for in vivo effects. This prodrug-like pharmacokinetics means many activities attributed to icariin are mediated by its deglycosylated metabolites.
What does the clinical evidence say about Icariin and bone health?
A 24-month randomized, double-blind, placebo-controlled trial (Zhang G et al., J Bone Miner Res 2007) in late postmenopausal women found Epimedium-derived flavonoids preserved femoral neck BMD (+1.6% vs -1.8% placebo) and lumbar spine BMD (+1.3% vs -2.4% placebo). Mechanistically, icariin promotes osteoblast differentiation through Wnt/β-catenin and BMP2/Runx2 signaling.
How should Icariin be dissolved and stored for research use?
Icariin is soluble in DMSO and ethanol and poorly soluble in water. Prepare a concentrated DMSO stock for cell-based assays, keeping final DMSO ≤0.1% v/v. Store the powder and stock solutions at 2-8°C, protected from light. Always research-use-only; not for human or clinical consumption.
Which signaling pathways does Icariin modulate?
Icariin engages a coordinated network: PDE5/cGMP for vascular relaxation, ERα/ERβ as a phytoestrogen, PPARα for lipid metabolism, and the Wnt/β-catenin plus BMP2/Runx2 axis for osteoblast differentiation. It also activates the Nrf2 antioxidant pathway and suppresses neuroinflammation, accounting for its broad research relevance.
Is QC documentation provided with each batch?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity (≥98%), NMR structural confirmation, and MS data. MSDS/SDS, solubility datasheets, and Certificates of Origin are available on request. Qualified institutions may request sample evaluation — please contact us for details.

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