| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
The primary target of MRS928 is the adenosine A3 receptor (A3R). It is a potent and selective antagonist at this receptor. It also inhibits TNF-α-induced MMP-1 expression and secretion. As a flavonoid, it has antioxidant properties.
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|---|---|
| ln Vitro |
In vitro, MRS928 inhibits TNF-α-induced MMP-1 expression and secretion in cells. It exhibits anti-inflammatory and anticancer properties. It has antioxidant activity. As an A3R antagonist, it modulates purinergic signaling.
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| ln Vivo |
In vivo, MRS928 has potential therapeutic applications due to its anti-inflammatory and anticancer properties. It may be useful for improving skin damage. Detailed in vivo data are available from research publications.
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| Enzyme Assay |
For in vitro assays, MRS928 is tested for its ability to inhibit TNF-α-induced MMP-1 expression. Standard protocols involve treating cells with TNF-α in the presence of varying concentrations of MRS928 (0.1-100 µM) and measuring MMP-1 levels by ELISA or Western blot.
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| Cell Assay |
Cell-based assays for MRS928 involve treating cells (e.g., fibroblasts or cancer cell lines) with the compound at concentrations of 0.1-100 µM for 24-72 hours. Anti-inflammatory activity is assessed by measuring cytokine or MMP levels. Anticancer activity is assessed by MTT assays for cell viability.
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| Animal Protocol |
In vivo studies with MRS928 are conducted in animal models of inflammation or cancer. Typical protocols involve administering the compound orally or intraperitoneally at doses of 1-50 mg/kg. Efficacy is assessed by measuring inflammatory markers or tumor growth.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MRS928 have been characterized in preclinical studies. As a flavonoid, it is likely to have reasonable bioavailability. Detailed PK parameters are available from research publications.
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| Toxicity/Toxicokinetics |
Toxicology data for MRS928 are available from preclinical studies. The compound is generally well-tolerated at therapeutic doses. As a natural product derivative, it has a favorable safety profile.
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| References | |
| Additional Infomation |
Galangin 3,5,7-trimethyl ether is a trimethoxyflavonoid, a 3,5,7-trimethyl ether derivative of galangin. It is a plant metabolite functionally related to galangin. 3,5,7-Trimethoxyflavonoids have been reported to exist in turmeric (Boesenbergia rotunda), kaempferia parviflora, and other organisms with relevant data.
MRS928 is 3,5,7-trimethoxyflavone, a flavonoid compound derived from galangin. It is a potent and selective A3 adenosine receptor antagonist. It has anti-inflammatory and anticancer properties. It inhibits TNF-α-induced MMP-1 expression. No FDA approvals exist. |
| Molecular Formula |
C18H16O5
|
|---|---|
| Molecular Weight |
312.32
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| Exact Mass |
312.1
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| CAS # |
26964-29-4
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| PubChem CID |
117900
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| Appearance |
Off-white to light yellow solid powder
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| Vapour Pressure |
1.22E-10mmHg at 25°C
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| LogP |
3.485
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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 |
4
|
| Heavy Atom Count |
23
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| Complexity |
466
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CBTHKWVPSIGKMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16O5/c1-20-12-9-13(21-2)15-14(10-12)23-17(18(22-3)16(15)19)11-7-5-4-6-8-11/h4-10H,1-3H3
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| Chemical Name |
3,5,7-trimethoxy-2-phenylchromen-4-one
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| Synonyms |
MRS-928; MRS 928; MRS928
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.2018 mL | 16.0092 mL | 32.0184 mL | |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 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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