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Chemical Structure| 489-32-7 Chemical Structure| 489-32-7

Structure of Icariin
CAS No.: 489-32-7

Chemical Structure| 489-32-7

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Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold selective for PDE5 than PDE4 and exhibits multiple biological properties, including anti-inflammatory, neuroregulatory and neuroprotective activities. It is a major constituent of flavonoids from the Chinese medicinal herb Epimedium brevicornum..

Synonyms: Ieariline

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Product Details of Icariin

CAS No. :489-32-7
Formula : C33H40O15
M.W : 676.66
SMILES Code : O=C1C(O[C@@H]2O[C@@H](C)[C@@H]([C@H]([C@H]2O)O)O)=C(C3=CC=C(OC)C=C3)OC4=C(C/C=C(C)\C)C(O[C@@H]5O[C@@H]([C@H]([C@@H]([C@H]5O)O)O)CO)=CC(O)=C14
Synonyms :
Ieariline
MDL No. :MFCD00210516
InChI Key :TZJALUIVHRYQQB-XLRXWWTNSA-N
Pubchem ID :5318997

Safety of Icariin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • PDE5

    PDE5, IC50:0.432 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
HMC3 cells 10 μM 24 h To investigate the effect of ICA on M1/M2 phenotypic polarization in HMC3 cells. Results showed that ICA significantly reduced the expression of M1 markers (TNF-α, COX-2, NO) and increased the expression of M2 markers (ARG1, CD206, IL-10). PMC8956882
Primary rat midbrain neuron-enriched cultures 0.1 μM 7 days To evaluate the protective effect of ICA on 6-OHDA-induced DA neuronal injury, results showed that ICA did not exhibit neuroprotection in neuron-enriched cultures. PMC6477740
Primary rat midbrain neuron-glia co-culture 0.1 μM 7 days To evaluate the protective effect of ICA on 6-OHDA-induced DA neuronal injury, results showed that ICA significantly attenuated 6-OHDA-induced DA neuronal injury in neuron-glia co-cultures. PMC6477740
H9c2 cells 4 μM 2 h To investigate the protective role of icariin via SIRT1 pathway in H9c2 cells, results demonstrated icariin pretreatment significantly enhanced cell survival and reduced apoptosis and necrosis markers. PMC6177614
Neonatal rat ventricular myocytes (NRVMs) 2, 4, 8 μM 12 h To evaluate the regulatory effect of icariin on SIRT1, results showed icariin significantly increased SIRT1 expression and dose-dependently improved cell viability post-SI/R injury, reducing apoptosis and necrosis. PMC6177614
4T1 20 μM 24 hours To evaluate the inhibitory effect of icariin on breast cancer cell proliferation, results showed that icariin significantly inhibited the proliferation of 4T1 cells. PMC7648025
MDA-MB-231 10 or 20 μM 24 hours To evaluate the inhibitory effect of icariin on breast cancer cell proliferation, results showed that icariin significantly inhibited the proliferation of MDA-MB-231 cells. PMC7648025

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Experimental autoimmune uveitis (EAU) model Intragastric administration 10 mg/kg Once daily for 7 days To investigate the effect of ICA on intraocular inflammation in EAU mice. Results showed that ICA significantly reduced conjunctival and ciliary hyperaemia and infiltration of anterior chamber inflammatory cells, decreased retinal folds and inflammatory cells, and improved the integrity of the blood-retinal barrier. PMC8956882
Mice 6-OHDA-induced Parkinson's disease model Intragastric administration 60 mg/kg Once daily for 10 consecutive days To evaluate the protective effect of ICA on 6-OHDA-induced DA neuronal injury, results showed that ICA attenuated 6-OHDA-induced DA neurotoxicity and glial cells-mediated neuroinflammatory response. PMC6477740
C57BL/6 mice Myocardial ischemia/reperfusion injury model Oral gavage 60 mg/kg Twice daily for 2 weeks To assess the cardioprotective effects of icariin against myocardial I/R injury, results showed icariin significantly improved cardiac function (EF and FS), reduced infarct size and apoptosis, and attenuated oxidative stress markers. PMC6177614

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01979133 Bipolar Disorder|Substance Use... More >> Disorder Less << PHASE3 COMPLETED 2025-06-15 The University of Texas Southw... More >>estern Medical Center, Dallas, Texas, 75390-8849, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.48mL

0.30mL

0.15mL

7.39mL

1.48mL

0.74mL

14.78mL

2.96mL

1.48mL

References

 

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