| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 52.50 μM (ACE)[1]
Angiotensin-converting enzyme (ACE) |
|---|---|
| ln Vitro |
The inhibitory activities of the target-isolated C-glycosylflavone (Vicenin 1) are assessed. Vicenin 1 has an IC50 value of 52.50 μM and demonstrates effective ACE inhibitory activities. Through the formation of chelate complexes inside the ACE active center, compound 3 (vicenin 1) under test exhibits activity[1].
Vicenin-1 displays effective ACE inhibitory activity with an IC50 of 52.50 microM. It exhibits notable antioxidant, anti-inflammatory, and cytoprotective properties, protecting against oxidative stress and inhibiting pro-inflammatory mediators. |
| ln Vivo |
Currently, no specific in vivo data is available for this compound. General in vivo information for similar flavonoids may include bioavailability studies and antioxidant efficacy in animal models.
|
| Enzyme Assay |
A typical enzyme inhibition assay protocol involves incubating the compound with ACE enzyme and a substrate, such as hippuryl-histidyl-leucine. The reaction is initiated, incubated at 37degC, and terminated by adding acid. The product is extracted and quantified by spectrophotometry to calculate inhibition percentage and IC50.
|
| Cell Assay |
A common in vitro protocol uses cell lines like human umbilical vein endothelial cells (HUVECs) or macrophage cells. Cells are treated with the compound and then stimulated with LPS or other inflammatory agents. Cell viability is measured by MTT assay, and inflammatory markers such as TNF-alpha, IL-6, and NO are quantified by ELISA.
|
| Animal Protocol |
For in vivo studies in rodents, general procedures include administering the compound via oral gavage or intravenous injection. In a hypertension model, blood pressure is monitored via tail-cuff. In an inflammation model, paw edema is measured after carrageenan injection. Tissues and blood are collected for histopathological and biochemical analysis.
|
| ADME/Pharmacokinetics |
General PK properties for similar flavonoids often indicate low oral bioavailability due to poor solubility and extensive metabolism, with a short half-life (t1/2). Plasma protein binding is typically high, and major metabolic pathways include glucuronidation and sulfation.
|
| Toxicity/Toxicokinetics |
General safety data for similar flavonoids suggest low acute toxicity, with an oral LD50 often >2000 mg/kg in rodents. Repeated dose studies may show no significant organ toxicity at therapeutic doses. However, due to its flavonoid nature, potential for drug-drug interactions through CYP enzyme modulation exists.
|
| References | |
| Additional Infomation |
According to reports, flax (Linum grandiflorum) contains vesinin-1, and there is relevant data.
Vicenin-1 functions by forming chelate complexes within the active center of ACE, leading to its inhibition. No clinical trials or approved drugs have been developed from Vicenin-1. |
| Molecular Formula |
C26H28O14
|
|---|---|
| Molecular Weight |
564.49
|
| Exact Mass |
564.148
|
| CAS # |
35927-38-9
|
| PubChem CID |
13644663
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.766±0.06 g/cm3
|
| Melting Point |
230 ºC (decomp)
|
| LogP |
-2.2
|
| Hydrogen Bond Donor Count |
10
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
40
|
| Complexity |
938
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
C1[C@H]([C@@H]([C@H]([C@@H](O1)C2=C(C(=C3C(=C2O)C(=O)C=C(O3)C4=CC=C(C=C4)O)[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O)O)O)O)O
|
| InChi Key |
OVMFOVNOXASTPA-MCIQUCDDSA-N
|
| InChi Code |
InChI=1S/C26H28O14/c27-6-13-18(32)21(35)23(37)26(40-13)16-20(34)15(25-22(36)17(31)11(30)7-38-25)19(33)14-10(29)5-12(39-24(14)16)8-1-3-9(28)4-2-8/h1-5,11,13,17-18,21-23,25-28,30-37H,6-7H2/t11-,13-,17+,18-,21+,22-,23-,25+,26+/m1/s1
|
| Chemical Name |
5,7-dihydroxy-2-(4-hydroxyphenyl)-8-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]-6-[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yl]chromen-4-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (177.15 mM)
|
|---|---|
| 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 | 1.7715 mL | 8.8576 mL | 17.7151 mL | |
| 5 mM | 0.3543 mL | 1.7715 mL | 3.5430 mL | |
| 10 mM | 0.1772 mL | 0.8858 mL | 1.7715 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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