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Hypericin

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Catalog No. T6S0923Cas No. 548-04-9
Alias Hypericine, Cyclosan

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

Hypericin

Hypericin

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🥰Excellent
Purity: 99.51%
Catalog No. T6S0923Alias Hypericine, CyclosanCas No. 548-04-9
Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$52In StockIn Stock
5 mg$129In StockIn Stock
10 mg$192In StockIn Stock
25 mg$379In StockIn Stock
50 mg$559In StockIn Stock
100 mg$783In StockIn Stock
500 mg$1,590In StockIn Stock
1 mL x 10 mM (in DMSO)$143In StockIn 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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Purity:99.51%
Color:Purple to Black
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Product Introduction

Hypericin AI Summary
Hypericin exhibits a broad spectrum of bioactivities across various biological targets. It inhibits HIV-1 integrase, specifically at the 3''-preprocessing step, with an IC50 of 10000 nM, indicating its potency against the enzyme related to HIV-1. The compound has a partition coefficient (logP) of 5.02, shows antioxidant potential (reducing activity against DPPH with kDPPH = 3.66 M-1 s-1), and peroxidant properties (malondialdehyde and deoxyribose release ratio < 0.3). In cytotoxicity assays, Hypericin exhibits antiproliferative activity against HaCaT cells (IC50 = 1700 nM) and significant cytotoxicity at 2 µM (LDH release = 159 MU). It also displays antidepressant activity in rats, binding to the dopamine D3 receptor (Ki = 34.5 nM) and inhibiting CRF1 receptor (IC50 = 300 nM), while reducing CRF mRNA and 5HT1A receptor mRNA expression. Additionally, it moderately inhibits CYP3A4 enzyme activity. The compound demonstrates antiviral activity against various viruses, including equine infectious anemia virus (EIAV) and SARS-CoV-2, with potent inhibition rates and IC50 values (SARS-CoV-2 IC50 = 250 nM). It also shows activity against Streptococcus mutans with a MIC of 250 µg/mL and ability to inhibit biofilm formation and decrease membrane fluidity. Furthermore, Hypericin inhibits multiple enzymes, including Hepatitis C virus NS3 helicase (IC50 = 3000 nM), sGC (IC50 = 200-700 nM), and HDAC6 (high inhibition percentages in various assays). It affects metabolic enzymes such as rat liver cytosolic TrxR1 (IC50 = 198000 nM), mitochondrial TrxR2 (IC50 = 49000 nM), and yeast glutathione reductase (IC50 = 3670 nM). The compound also inhibits acetylcholinesterase and butyrylcholinesterase. Additionally, it shows bioactivity in decreasing cellular cGMP levels in frog atrial myocytes at 4 µM, inhibiting alpha-synuclein filament formation (IC50 = 7500 nM), and maintaining stability with a human half-life of 42 hours, clearance rate of 0.13 mL/min/kg, and volume of distribution at steady state of 0.25 L/kg. Overall, Hypericin represents a multipotent bioactive compound with potential therapeutic applications across various diseases, including viral infections, cancer, neurological disorders, and more..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.
Targets&IC50
Y2 receptor:3-4 μM, Hvr100-6:22.9 ± 1.4 mM, NPYY1 receptor:3-4 μM, HeLa cells:17.2 ± 3.3 mM, melanocytes:3.5 μM (LD50), Fibroblasts:1.75 μM (LD50), keratinocytes:4 μM (LD50), Tyrosine kinase:7.5 μM, MCF-7 cells:5 µg/mL (LD50)
In vitro
METHODS: Erythrocytes were treated with Bioymifi (10-100 µM) for 24 h. Flow cytometry was used to characterize the hemolytic and bactericidal properties of Bioymifi and the potential molecular mechanisms.
RESULTS: Bioymifi exerted a dose-responsive, calcium-independent hemolytic effect, reduced erythrocyte hemoglobin, and significantly increased membrane-bound protein V, Fluo4, and DCF-positive cells, as well as a dual effect on forward and lateral light scattering. [1]
METHODS: Neonatal rat ventricular myocytes (nrvm) were treated with Bioymifi (10 µM) for 24 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: The expression of DR5 was higher than that of NRVF in Bioymifi-treated nrvm. [2]
In vivo
METHODS: To investigate the role of DR5 activation in the heart, Bioymifi (5 mg/kg/d) micro-osmotic pump was administered to C57BL/6 mice once daily for two weeks.
RESULTS: Bioymifi administration resulted in hypertrophy at the level of cardiac organs and cardiomyocytes, but did not affect cardiomyocyte death or cardiac fibrosis. [2]
SynonymsHypericine, Cyclosan
Chemical Properties
Molecular Weight504.44
FormulaC30H16O8
Cas No.548-04-9
SmilesCc1cc(O)c2c3c1c1c(C)cc(O)c4c1c1c3c3c(c(O)cc(O)c3c2=O)c2c(O)cc(O)c(c12)c4=O
Relative Density.1.915 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 5 mg/mL (9.91 mM), Heating is recommended.
DMSO: 100 mg/mL (198.24 mM), Sonication is recommended.
Propylene glycol: 2.52 mg/mL (5 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.25 mg/mL (2.48 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
Propylene glycol/Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.9824 mL9.9120 mL19.8240 mL99.1198 mL
5 mM0.3965 mL1.9824 mL3.9648 mL19.8240 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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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

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