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Icariin

Name: Icariin
Brand: TargetMol
SKU: T2855
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2855Cas No. 489-32-7

Alias Ieariline

Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432/73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.

Icariin

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Purity: 98.3%

Catalog No. T2855Alias IearilineCas No. 489-32-7

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$33	In Stock	In Stock
100 mg	$47	In Stock	In Stock
200 mg	$67	In Stock	In Stock
500 mg	$107	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$52	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.3%

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Icariin AI Summary

Icariin exhibits a wide range of bioactivities and pharmacological properties. It functions as an inhibitor of several enzymes and transporters, including human recombinant PDE5A1 (IC50 of 5900 nM), human PDE6C (45.0% inhibition at 10 µM), DNA Polymerase Beta (potency of 63095.7 nM), Human Apurinic/apyrimidinic Endonuclease 1 (APE1) (potency of 11220.2 nM), and LSD1 (IC50 of 26440.0 nM). It also inhibits sodium fluorescein uptake in OATP1B1-transfected CHO cells by 212.53% and OATP1B3-transfected CHO cells by 126.78% at 10 µM concentration. The compound has demonstrated bioactivity in reversing P-gp-mediated multidrug resistance in human MCF7/ADR cells and exhibited cytotoxicity against these cells with an IC50 greater than 100,000 nM after 72 hours. In mouse TM3 cells, Icariin showed cytotoxicity with a CC50 value greater than 200,000 nM and induced testosterone production, leading to a 139.6% increase at 20 µM. In terms of antiviral activity, Icariin inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells (7.62% inhibition at 10 µM after 48 hours) and VERO-6 cells (0.08% inhibition at 10 µM after 48 hours). It also shows 11.86% inhibition of SARS-CoV-2 3CL-Pro protease activity at 20 µM. Furthermore, the compound exhibits modest antifungal activity against Candida albicans (inhibition of 4.36%) and Cryptococcus neoformans (inhibition of 0.11%), and varying antibacterial activity, including 19.01% inhibition against Acinetobacter baumannii and 18.03% against Pseudomonas aeruginosa. Icariin also demonstrates significant inhibitory activity against human IDH1 R132H mutant and wild-type IDH1, with 103.8% and 90.4% activity, respectively, using spectrophotometry measurements..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432/73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.
Targets&IC50	PDE4:73.5 μM, PDE5:0.432 μM
In vitro	METHODS: Osteoarthritic fibroblast-like synoviocytes OA-FLSs were treated with Icariin (0.1-10 µM) for 12 h, and cell viability was measured using MTS assay. RESULTS: No cytotoxic effect of Icariin at 0.1-1 µM was observed in OA-FLSs. At a concentration of 10 µM, Icariin showed low cytotoxicity to OA-FLSs, which significantly inhibited the proliferation of OA-FLSs after 12 h. The results showed that Icariin was not effective in inhibiting the proliferation of OA-FLSs after 12 h of treatment. [1] METHODS: Fibroblast-like synoviocyte FLSs were treated with Icariin (1-5 µM) for 24-36 h. Cell migration was detected using the Wounding migration assay and Transwell chamber assay. RESULTS: Wound closure was significantly slowed in FLS treated with Icariin, and Transwell chamber assay showed that Icariin inhibited FLS migration in a concentration-dependent manner. [2]
In vivo	METHODS: To investigate the protective effects against traumatic brain injury (TBI), Icariin (3-30 mg/kg) was administered orally twice daily for seven days to a mouse model of TBI induced by controlled cortical impact. RESULTS: The Icariin 30 mg/kg and 10 mg/kg treatment groups showed enhanced sensorimotor function 8 days after TBI in the rotating bar and balance beam tests.The Icariin treatment group showed an increase in recognition indices in the novel object recognition test at all doses, and an increase in spontaneous alternation in the Y maze test in the 30 mg/kg group.Icariin upregulated the expression of brain-derived neurotrophic factor, synaptophysin, and postsynaptic density protein 95. However, no protective effect against brain injury or neuronal death was observed. [3]
Synonyms	Ieariline

Chemical Properties

Molecular Weight	676.66
Formula	C₃₃H₄₀O₁₅
Cas No.	489-32-7
Smiles	COC1=CC=C(C=C1)C1=C(O[C@@H]2O[C@@H](C)[C@H](O)[C@@H](O)[C@H]2O)C(=O)C2=C(O)C=C(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)C(CC=C(C)C)=C2O1
Relative Density.	1.55 g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 245 mg/mL (362.07 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 6 mg/mL (8.87 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4778 mL	7.3892 mL	14.7785 mL	73.8924 mL
5 mM	0.2956 mL	1.4778 mL	2.9557 mL	14.7785 mL
10 mM	0.1478 mL	0.7389 mL	1.4778 mL	7.3892 mL
20 mM	0.0739 mL	0.3695 mL	0.7389 mL	3.6946 mL
50 mM	0.0296 mL	0.1478 mL	0.2956 mL	1.4778 mL
100 mM	0.0148 mL	0.0739 mL	0.1478 mL	0.7389 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc