| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Monascin targets multiple pathways involved in metabolism, inflammation, and cancer. It is a PPARγ agonist, activating peroxisome proliferator-activated receptor gamma, which regulates glucose and lipid metabolism and improves insulin sensitivity. It activates the Nrf2 pathway, enhancing antioxidant defense and reducing oxidative stress. It inhibits the activation of NOR 1 (an NO donor). It attenuates proinflammatory mediators, including iNOS and COX-2 expression as well as NO and PGE2 formation. Its antitumor activity is mediated through multiple mechanisms including inhibition of tumor initiation and induction of cell death.
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| ln Vitro |
In vitro, Monascin has demonstrated potent antitumor activity, notably against lung adenocarcinoma (LUAD) A549 cells with an IC50 of 2.05 µM. It has anti-inflammatory activity, attenuating proinflammatory mediators including iNOS and COX-2 expression as well as NO and PGE2 formation. It acts as a PPARγ agonist, improving hyperglycemia and insulin sensitivity. It activates the Nrf2 pathway. These activities confirm its potential for cancer, inflammation, and metabolic disease research.
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| ln Vivo |
Monascus (0.0025% in drinking water; mice) seems to be useful in preventing skin cancer in mice caused by UVB rays [1].
In vivo, Monascin (0.0025% in drinking water) appears effective for the inhibition of UVB-initiated carcinogenesis on mouse skin. It has anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Its PPARγ agonist activity improves hyperglycemia and insulin sensitivity in animal models. Its Nrf2 activating properties contribute to its antioxidant and anti-inflammatory effects in vivo. These in vivo effects support its potential for cancer prevention, inflammation, and metabolic disease treatment. |
| Enzyme Assay |
For in vitro biochemical assays, Monascin is evaluated for its PPARγ agonist and Nrf2 activator activities. PPARγ activation is assessed using cell-free transcription assays with purified receptor and response elements. Nrf2 activation is assessed by measuring the expression of Nrf2 target genes or by measuring Nrf2 protein levels. Anti-inflammatory activity is assessed by measuring inhibition of iNOS, COX-2, NO, and PGE2. Antioxidant activity is measured using DPPH, ABTS, or FRAP assays. Antitumor activity is assessed using cell viability and proliferation assays. These cell-free and cell-based assays help characterize the compound's multiple biological activities.
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| Cell Assay |
In vitro cellular assays for Monascin are performed using various cell types including cancer cells (A549), immune cells, and adipocytes. Cells are cultured in standard media and treated with the compound at various concentrations. Cell viability is assessed using MTT or SRB assays, with an IC50 of 2.05 µM against A549 cells. PPARγ activation is assessed by measuring the expression of PPARγ target genes. Nrf2 activation is assessed by measuring Nrf2 target gene expression. Anti-inflammatory activity is assessed by measuring iNOS, COX-2, NO, and PGE2 levels. These cellular assays help validate the compound's antitumor, anti-inflammatory, and metabolic activities.
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| Animal Protocol |
Animal/Disease Models: SENCAR mice, using UVB irradiation as the initiator and TPA as the promoter [1].
Doses: 0.0025% in drinking water. Route of Administration: Take orally with drinking water daily for 2 weeks Experimental Results: diminished number of papillomas. In vivo animal experiments with Monascin are conducted in models of cancer, inflammation, and metabolic diseases. For cancer studies, UVB-initiated carcinogenesis on mouse skin is used, with Monascin administered in drinking water (0.0025%). For metabolic studies, models of diabetes or obesity are used. For anti-inflammatory studies, models of inflammation are used. Monascin is administered orally. Efficacy endpoints include tumor incidence, inflammation markers, blood glucose levels, and insulin sensitivity. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Monascin have been partially characterized. As an azaphilonoid pigment with a molecular weight of 358.43, it is expected to have moderate oral bioavailability. The compound is soluble in organic solvents. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are not extensively documented. The compound should be stored under recommended conditions to maintain stability.
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| Toxicity/Toxicokinetics |
The toxicological profile of Monascin is not extensively characterized. As a natural pigment from Monascus-fermented rice, it is generally considered to have a favorable safety profile, but comprehensive toxicity studies are limited. The compound is intended for research use only and not for human therapeutic applications. Its effects at high concentrations and potential interactions with other drugs or compounds have not been fully investigated. Researchers should follow standard laboratory safety practices when handling Monascin.
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| References |
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| Additional Infomation |
Monascin is an organic heterocyclic tricyclic compound with the chemical formula 3a,4,8,9a-tetrahydro-2H-furano[3,2-g][2]benzopyran-2,9(3H)-dione, in which the 3, 6, and 9a positions are substituted with hexanoyl, (1E)-prop-1-en-1-yl, and methyl groups, respectively (3S,3aR,9aR diastereomers). It is a phenanthrene ketone pigment found in the extract of Monascus purpureus fermented rice (red yeast rice), and exhibits significant inhibitory effects on chemically or ultraviolet-induced, phorbol-promoted mouse skin tumors. It also possesses antitumor activity, PPARγ agonist activity, lipid-lowering activity, and fungal metabolite activity. It is an organic heterocyclic tricyclic compound belonging to the γ-lactone, α,β-unsaturated ketone, and polyketide compounds. Monascin has been reported to be present in Monascus purpureus, Monascus trichomoniata, and Monascus purpureus, and relevant data are available.
Monascin is a valuable research tool for studying PPARγ activation, Nrf2 activation, and anti-inflammatory mechanisms. Its PPARγ agonist activity makes it useful for investigating glucose and lipid metabolism and developing treatments for diabetes and metabolic syndrome. Its Nrf2 activation provides opportunities for studying antioxidant defense and developing therapies for oxidative stress-related diseases. Its antitumor activity against lung adenocarcinoma cells (IC50 = 2.05 µM) makes it relevant for cancer research. As a pigment from Monascus-fermented rice, it is also important for food science and natural product chemistry. |
| Molecular Formula |
C21H26O5
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| Molecular Weight |
358.4281
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| Exact Mass |
358.178
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| CAS # |
21516-68-7
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| PubChem CID |
12118082
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| Appearance |
Light yellow to yellow solid
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| LogP |
3.443
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
727
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O1C([C@]([H])(C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)[C@@]2([H])C([H])([H])C3C([H])=C(/C(/[H])=C(\[H])/C([H])([H])[H])OC([H])([H])C=3C([C@]12C([H])([H])[H])=O)=O
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| InChi Key |
XXKNHBAFFJINCK-RVEJDSBJSA-N
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| InChi Code |
InChI=1S/C21H26O5/c1-4-6-7-9-17(22)18-16-11-13-10-14(8-5-2)25-12-15(13)19(23)21(16,3)26-20(18)24/h5,8,10,16,18H,4,6-7,9,11-12H2,1-3H3/b8-5+/t16-,18+,21-/m1/s1
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| Chemical Name |
(3S,3aR,9aR)-3-hexanoyl-9a-methyl-6-[(E)-prop-1-enyl]-3,3a,4,8-tetrahydrofuro[3,2-g]isochromene-2,9-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~139.50 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7899 mL | 13.9497 mL | 27.8995 mL | |
| 5 mM | 0.5580 mL | 2.7899 mL | 5.5799 mL | |
| 10 mM | 0.2790 mL | 1.3950 mL | 2.7899 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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