Art. -Nr.: HY-N0014

Icariin

Name: Icariin
Brand: MedChemExpress
SKU: HY-N0014
Price: 60.00 USD
Availability: InStock
Rating: 5 (31 reviews)

(Synonyms: Ieariline)

31 Cited Publications

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Based on 31 publication(s) in Google Scholar

Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC₅₀s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

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Reinheit : 98.95%
CAS. Nr.: 489-32-7
Formel: C₃₃H₄₀O₁₅
Molecular Weight:676.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Icariin Chemical Structure

CAS. Nr.: 489-32-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (31)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC₅₀s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

IC₅₀ & Target

^[1]^[2]

PDE5

432 nM (IC₅₀)

PDE4

73.5 μM (IC₅₀)

PPARα

Autophagy

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

Alle PPAR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	5.9 μM Compound: 1	Inhibition of human recombinant PDE5A1 expressed in COS7 cells Inhibition of human recombinant PDE5A1 expressed in COS7 cells	[PMID: 18778098]
NCI/ADR-RES	IC₅₀	>100 μM Compound: 1, icariin	Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay	[PMID: 19523827]
TM3	CC₅₀	>200 μM Compound: Icariin	Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay	[PMID: 31091478]

In Vitro

Icariin is a cGMP-specific PDE5 inhibitor. The inhibitory effects of Icariin on PDE5 and PDE4 activities are investigated by the two-step radioisotope procedure with ³H-cGMP/³H-cAMP. The potency of selectivity of Icariin on PDE5 (PDE4/PDE5 of IC₅₀) is 167.67 times^[1]. Cell viability is measured in the present study to evaluate whether Icariin protect endothelial HUVECs from injuries induced by oxidized low-density lipoprotein (ox-LDL). The exposure of the cells to ox-LDL for 24 h significantly decreases the cell viability compared with control group (P<0.05). However, Icariin can inhibit cell injury induced by ox-LDL in a concentration-dependent manner, and has significant difference (P<0.05) compared with ox-LDL-simulated group^[3].
Icariin protects BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

Icariin is a PPARα activator, induces Cyp4a10 and Cyp4a14, and regulates the mRNA levels of lipid metabolism enzymes and proteins, including fatty acid binding protein, fatty acid oxidation in mitochondria and in peroxisome. Icariin is effective in the treatment of hyperlipidemia. To understand the effect of Icariin on lipid metabolism, effects of Icariin on PPARα and its target genes are investigated. Mice are treated orally with Icariin at doses of 0, 100, 200, and 400 mg/kg, or Clofibrate (500 mg/kg) for five days. Liver total RNA is isolated and the expressions of PPARα and lipid metabolism genes are examined. PPARα and its marker genes Cyp4a10 and Cyp4a14 are induced 2-4 fold by Icariin, and 4-8 fold by Clofibrate. The fatty acid (FA) binding and co-activator proteins Fabp1, Fabp4 and Acsl1 are increased 2-fold. The mRNAs of mitochondrial FA β-oxidation enzymes (Cpt1a, Acat1, Acad1 and Hmgcs2) are increased 2-3 fold. The mRNAs of proximal β-oxidation enzymes (Acox1, Ech1, and Ehhadh) are also increased by Icariin and Clofibrate. The expression of mRNAs for sterol regulatory element-binding factor-1 (Srebf1) and FA synthetase (Fasn) are unaltered by Icariin. The lipid lysis genes Lipe and Pnpla2 are increased by Icariin and Clofibrate^[2]. Adult rats are treated orally with Icariin at doses of 0 (control), 50, 100, or 200 mg/kg body weight for 35 consecutive days. The results show that Icariin has virtually no effect on the body weight or organ coefficients of the testes or epididymides. However, 100 mg/kg Icariin significantly increases epididymal sperm counts. In addition, 50 and 100 mg/kg Icariin significantly increase testosterone levels. Furthermore, 100 mg/kg Icariin treatment also affects follicle stimulating hormone receptor (FSHR) and claudin-11 mRNA expression in Sertoli cells. Superoxide dismutase (SOD) activity and malondialdehyde (MDA) levels are measured in the testes; 50 and 100 mg/kg Icariin treatment improve antioxidative capacity, while 200 mg/kg Icariin treatment upregulates oxidative stress^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 489-32-7
Appearance Solid
Molecular Weight 676.66
Formel C₃₃H₄₀O₁₅
Color Light yellow to yellow
SMILES

O[C@H]1[C@H](O)[C@@H](CO)O[C@@H](OC2=C(C/C=C(C)/C)C(OC(C3=CC=C(OC)C=C3)=C(O[C@@H]4O[C@@H](C)[C@H](O)[C@@H](O)[C@H]4O)C5=O)=C5C(O)=C2)[C@@H]1O
Synonyms

Ieariline
Structure Classification
- Flavonoids
- Flavonols
- Phenols
- Monophenols
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (31)

All Cell Imaging/StainingWBCell Proliferation/Viability Assay

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Journal Impact Factor

Phytomedicine

Fangchinoline suppresses nasopharyngeal carcinoma progression by inhibiting SQLE to regulate the PI3K/AKT pathway dysregulation. [Abstract]

2025 May:140:156484. PMID: 40090046
Phytomedicine

Icariin protects against acute graft-versus-host disease while preserving graft-versus-leukemia activity after allogeneic hematopoietic stem cell transplantation. [Abstract]

2024 Sep:132:155901. PMID: 39067193
Food Chem

Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]

2025 Dec 30:497:146992. PMID: 41285060
Food Chem

Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]

2025 Oct 15:489:144992. PMID: 40466530
Regen Biomater

2026 Jul 3:13:rbag143. PMID: 42553951
Int J Biol Macromol

Natural angiotensin II type 1 receptor inhibitors: Virtual screening and in vitro evaluation of beta-1,2,3,4,6-penta-O-galloyl-d-glucopyranose, icarrin, and sesamin for osteoarthritis therapy. [Abstract]

2025 May;309(Pt 1):142184. PMID: 40147655
J Ethnopharmacol

Icariin maintaining TMEM119-positive microglial population improves hippocampus-associated memory in senescent mice in relation to R-3-hydroxybutyric acid metabolism. [Abstract]

2025 Jan 31:340:119287. PMID: 39736348
Biochem Pharmacol

2026 Oct:252:118212. PMID: 42398866
RSC Adv

Eco-benign spectrofluorimetric analysis of icariin in a nano-formulation using green quantum dots: insights from in vitro anticoagulant and docking studies. [Abstract]

2025 Sep 29;15(43):35971-35985. PMID: 41030304
Int Immunopharmacol

Icariin alleviates cardiomyocyte pyroptosis through AMPK-NLRP3 pathway to ameliorates diabetic cardiomyopathy. [Abstract]

2025 May 27:156:114690. PMID: 40262250
Int Immunopharmacol

Direct targeting of S100A9 with Icariin counteracted acetaminophen‑induced hepatotoxicity. [Abstract]

2024 Jul 30:136:112296. PMID: 38810310
Int J Mol Sci

Icariin Improves Stress Resistance and Extends Lifespan in Caenorhabditis elegans through hsf-1 and daf-2-Driven Hormesis. [Abstract]

2023 Dec 26;25(1):352. PMID: 38203522
Front Pharmacol

Icariin Ameliorates Diabetic Cardiomyopathy Through Apelin/Sirt3 Signalling to Improve Mitochondrial Dysfunction. [Abstract]

2020 Mar 19:11:256. PMID: 32265695

Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19:11:256. [Abstract]

As demonstrated by Masson staining, collagen deposition was reduced in the myocardium of Icariin (30 mg/kg)-treated db/db mice.

Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19:11:256. [Abstract]

The DHE staining indicated that Icariin (30 mg/kg) treatment alleviated the production of ROS in the myocardial tissue of db/db mice.

Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19:11:256. [Abstract]

TUNEL staining revealed that Icariin (30 mg/kg) treatment rescued the apoptotic rate of cardiomyocytes.

Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19:11:256. [Abstract]

The mitochondrial dynamics-related protein, Mfn2, mitochondrial biogenesis regulation protein, PGC‐1α, and mitochondrial gene, cytochrome-b (Cyt-b), were upregulated in the Icariin-treated (30 mg/kg) db/db mice.

Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19:11:256. [Abstract]

The number of HG-treated cardiomyocytes was significantly higher following incubation with Icariin for 12 h, 24 h, or 48 h at concentrations of 7.5, 15, or 30 µM.
Exp Neurol

Icariin attenuates oxidative stress via SIRT1/PGC-1α pathway in SAH mice. [Abstract]

2025 Aug:390:115303. PMID: 40345568
Cell Signal

Icariin attenuates premature ovarian insufficiency via a phytoestrogenic mechanism mediated by the ERβ/SIRT3 pathway. [Abstract]

2026 Mar:139:112334. PMID: 41421717
Brain Res Bull

Icariin promotes lysosomal degradation of amyloid-β precursor protein via enhanced endosome-lysosome trafficking to reduce amyloid-β accumulation and improve cognitive function in Alzheimer's disease models. [Abstract]

2026 Apr 27:111906. PMID: 42055146
Mol Divers

Investigating the molecular mechanism of epimedium herb in treating rheumatoid arthritis through network pharmacology, molecular docking, and experimental validation. [Abstract]

2025 Jan 16. PMID: 39821498
Front Biosci (Landmark Ed)

Icariin Attenuates Neuroinflammation and Dopaminergic Degeneration in a Rodent Model of Parkinson's Disease by Promoting the Expansion of Regulatory T Cells. [Abstract]

2026 Jun 26;31(6):47325. PMID: 42411473
J Orthop Surg Res

Investigation on the role of Icariin in tendon injury repair: focusing on tendon stem cell differentiation. [Abstract]

2025 Apr 15;20(1):379. PMID: 40234966
J Orthop Surg Res

Icariin promotes osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) by activating PI3K-AKT-UTX/EZH2 signaling in steroid-induced femoral head osteonecrosis. [Abstract]

2025 Mar 18;20(1):290. PMID: 40098175
J Orthop Surg Res

The SPI1/SMAD5 cascade in the promoting effect of icariin on osteogenic differentiation of MC3T3-E1 cells: a mechanism study. [Abstract]

2024 Jul 29;19(1):444. PMID: 39075522
J Pharm Pharmacol

Icariside I reduces breast cancer proliferation, apoptosis, invasion, and metastasis probably through inhibiting IL-6/STAT3 signaling pathway. [Abstract]

2024 May 3;76(5):499-513. PMID: 37971302
Toxicol Appl Pharmacol

Icariin regulates osteogenic/adipogenic differentiation of bone marrow mesenchymal stem cells in postmenopausal osteoporosis, potentially via the AMPK-mTOR-autophagy pathway. [Abstract]

2026 May:510:117761. PMID: 41702462
J Neurorestoratology

2025 Oct.
J Alzheimers Dis

Icariin improves learning and memory function by enhancing HRD1-mediated ubiquitination of amyloid precursor protein in APP/PS1 mice. [Abstract]

2025 Jan;103(2):616-626. PMID: 39814545
J Cell Biochem

Icariin promotes osteogenic differentiation of bone marrow stromal cells and prevents bone loss in OVX mice via activating autophagy. [Abstract]

2019 Aug;120(8):13121-13132. PMID: 30887562
Biochem Biophys Res Commun

Icariin alleviates cellular injury induced by cardiac ischemia-reperfusion injury by inhibiting IRE1/JNK-induced ferroptosis. [Abstract]

2024 Nov 12:733:150716. PMID: 39321486
Arch Dermatol Res

Icariin ameliorates TNF-α/IFN-γ-induced oxidative stress, inflammatory response and apoptosis of human immortalized epidermal cells through the WTAP/SERPINB4 axis. [Abstract]

2024 Aug 23;316(8):557. PMID: 39177922
Biochem Biophys Res Commun

Icariin inhibits RANKL-induced osteoclastogenesis in RAW264.7 cells via inhibition of reactive oxygen species production by reducing the expression of NOX1 and NOX4. [Abstract]

2022 Apr 16:600:6-13. PMID: 35182975
Turk J Gastroenterol

Icariin Inhibits Intestinal Inflammation of DSS-Induced Colitis Mice Through Modulating Intestinal Flora Abundance and Modulating p-p65/p65 Molecule. [Abstract]

2021 Apr;32(4):382-392. PMID: 34231485
Patent

US20230111925A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (147.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4778 mL

7.3892 mL

14.7785 mL

5 mM

0.2956 mL

1.4778 mL

2.9557 mL

10 mM

0.1478 mL

0.7389 mL

1.4778 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (3.07 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xin ZC, et al. Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8. [Content Brief]

[2]. Lu YF, et al. Icariin is a PPARα activator inducing lipid metabolic gene expression in mice. Molecules. 2014 Nov 6;19(11):18179-91. [Content Brief]

[3]. Hu Y, et al. Effects and mechanisms of icariin on atherosclerosis. Int J Clin Exp Med. 2015 Mar 15;8(3):3585-9. [Content Brief]

[4]. Chen M, et al. Effects of icariin on reproductive functions in male rats. Molecules. 2014 Jul 3;19(7):9502-14. [Content Brief]

[5]. Liu D, et al. Icariin protects rabbit BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated autophagy via MAPK signaling pathway. Life Sci. 2020 Apr 26:117730. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4778 mL	7.3892 mL	14.7785 mL	36.9462 mL
	5 mM	0.2956 mL	1.4778 mL	2.9557 mL	7.3892 mL
	10 mM	0.1478 mL	0.7389 mL	1.4778 mL	3.6946 mL
	15 mM	0.0985 mL	0.4926 mL	0.9852 mL	2.4631 mL
	20 mM	0.0739 mL	0.3695 mL	0.7389 mL	1.8473 mL
	25 mM	0.0591 mL	0.2956 mL	0.5911 mL	1.4778 mL
	30 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2315 mL
	40 mM	0.0369 mL	0.1847 mL	0.3695 mL	0.9237 mL
	50 mM	0.0296 mL	0.1478 mL	0.2956 mL	0.7389 mL
	60 mM	0.0246 mL	0.1232 mL	0.2463 mL	0.6158 mL
	80 mM	0.0185 mL	0.0924 mL	0.1847 mL	0.4618 mL
	100 mM	0.0148 mL	0.0739 mL	0.1478 mL	0.3695 mL

Bioz

Keywords

Icariin

31 Cited Publications

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Icariin

Publications Citing Use of MedChemExpress (MCE) Icariin

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Alle PPAR Isoform-spezifische Produkte anzeigen