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    Icariin (Ieariline)
    Icariin (Ieariline)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0786
    CAS #: 489-32-7Purity ≥98%

    Description: Icariin (also called Ieariline), a naturally occuring flavonol glycoside found in Epimedium (a Chinese medicinal herb), is a potent cGMP-specific Phosphodiesterase PDE5 inhibitor with important biological activity. It inhibits PDE5 with IC50 of 0.432 μM, and is 167-fold more selective for PDE5 over PDE4.  

    References: Asian J Androl. 2003 Mar;5(1):15-8.

    Related CAS: 113558-15-9 (Baohuoside I; Icariin-II; Icariside-II); 118525-35-2 (sagittatoside A; Icariin-A) ;  118525-36-3 (Sagittatoside B)

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    • 香港大学
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    Molecular Weight (MW)676.66
    CAS No.489-32-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 50 mg/mL (73.9 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/L
    Other info

    Icariin; Ieariline; 3-((6-Deoxymannopyranosyl)oxy)-7-(glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-4H-1-benzopyran-4-one;

    Chemical Name: 5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-7-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-3-(((2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4H-chromen-4-one 


    InChi Code: InChI=1S/C33H40O15/c1-13(2)5-10-17-19(45-33-28(42)26(40)23(37)20(12-34)46-33)11-18(35)21-24(38)31(48-32-27(41)25(39)22(36)14(3)44-32)29(47-30(17)21)15-6-8-16(43-4)9-7-15/h5-9,11,14,20,22-23,25-28,32-37,39-42H,10,12H2,1-4H3/t14-,20+,22-,23+,25+,26-,27+,28+,32-,33+/m0/s1

    SMILES Code: O=C1C(O[[email protected]]2[[email protected]@H]([[email protected]@H]([[email protected]]([[email protected]](C)O2)O)O)O)=C(C3=CC=C(OC)C=C3)OC4=C(C/C=C(C)\C)C(O[[email protected]]5[[email protected]@H]([[email protected]]([[email protected]@H]([[email protected]@H](CO)O5)O)O)O)=CC(O)=C14

    InChi Code: InChI=1S/C33H40O15/c1-13(2)5-10-17-19(45-33-28(42)26(40)23(37)20(12-34)46-33)11-18(35)21-24(38)31(48-32-27(41)25(39)22(36)14(3)44-32)29(47-30(17)21)15-6-8-16(43-4)9-7-15/h5-9,11,14,20,22-23,25-28,32-37,39-42H,10,12H2,1-4H3/t14-,20+,22-,23+,25+,26-,27+,28+,32-,33+/m0/s1
    SMILES Code: O=C1C(O[[email protected]]2[[email protected]@H]([[email protected]@H]([[email protected]]([[email protected]](C)O2)O)O)O)=C(C3=CC=C(OC)C=C3)OC4=C(C/C=C(C)\C)C(O[[email protected]]5[[email protected]@H]([[email protected]]([[email protected]@H]([[email protected]@H](CO)O5)O)O)O)=CC(O)=C14

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    In Vitro

    In vitro activity: Icariin inhibited the activity of PDE5 and PDE4 in a dose- andconcentration-dependent manner. The IC50of icariin on PDE5 was 0.43 µM and the IC50 on PDE4 was 73.50 µM. Icariin showed a selective inhibitory effect on cGMP-specific PDE5 compared to cAMP-specific PDE4. Icariincould also enhance the osteogenic differentiation of rat primary bone marrow stromal cells.

    Cell Assay: Human umbilical vein endothelial cells (HUVECs) in the logarithmic growth phase are seeded into 96-well plates at a density of 1×104 cells per well, then incubated for 24 hours at 37°C, 5% CO2. After pretreatment with indicated concentration of Icariin (0, 10, 20, 40 μM) for 24 hours, the cells are incubated with or without ox-LDL (100 μg/mL) for next 24 hours. After suction of the liquid in the wells, MTT solution is added to yield a final concentration of 0.5 mg/mL, and incubation is continued for 4 h at 37°C, 5% CO2. MTT solution is removed gently and 150 μL of DMSO is added to each well for 15 min incubation. The absorbance of each sample is measrured on a microplate reader at 490 nm as cell viability. 

    In VivoIn castrated rats, a 4-week oral administration of icariinat 1 mg/kg/day and 5 mg/kg/day improved the erectile function and increased nNOS and iNOS expression. Icariin also showed its effect on stimulating angiogenesis in human endothelial cells.
    Animal modelRats
    Formulation & DosageMice: Adult 8-week old male C57BL/6 mice are acclimated for 1-week in a temperature- and humidity-controlled facility with a standard 12-h light schedule. Mice have free access to SPF-grade rodent chow and purified drinking water. Mice are treated with Icariin (100, 200, and 400 mg/kg) for 5 days. Clofibrate (CLO, 500 mg/kg, po for 5 days) is used as a positive control, for negative controls, mice are given 2% CMC (10 mL/kg). 24 h after the last dose, livers are collected for analysis.

    Rats: Forty adult male SD rats weighing 200-290 g (12-16 weeks old) are randomly assigned to groups (n=10 per group) according to their body weight. The rats receive daily intragastric administration of Icariin at 0 (control), 50, 100, or 200 mg/kg per day for 35 consecutive days. The animals are weighed weekly, and the treatments are adjusted accordingly. At the end of the Icariin treatment period, all rats are sacrificed; blood samples are subsequently collected for further analyses of testosterone levels.

    References Asian J Androl. 2003 Mar;5(1):15-8; Biochem Biophys Res Commun. 2008 Nov 14;376(2):404-8; Molecules. 2014 Jul 3;19(7):9502-14.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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