| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Gentisin targets vascular smooth muscle cell proliferation. The compound's anti-proliferative effect has been confirmed by quantification of DNA synthesis (BrdU incorporation) in VSMC. Gentisin's mutagenic activity suggests it may interact with DNA. Its antioxidant, anti-inflammatory, and antimicrobial properties are mediated through multiple mechanisms. The compound's specific molecular targets are being elucidated through ongoing research.
|
|---|---|
| ln Vitro |
Gentisin is a novel inhibitor of vascular smooth muscle cell proliferation with an IC50 value of 7.84 μM. The anti-proliferative effect is confirmed by the quantification of DNA synthesis (BrdU incorporation) in VSMC. The compound exhibits antioxidant, anti-inflammatory, and antimicrobial properties in vitro. Gentisin has mutagenic activity, which has been demonstrated in various assays. Its effects on cell proliferation and DNA synthesis have been characterized in cellular models.
|
| ln Vivo |
Gentisin has been studied for its potential therapeutic applications in oxidative stress-related disorders. The compound's antioxidant, anti-inflammatory, and antimicrobial properties support its potential for various therapeutic applications. Its mutagenic activity suggests potential genotoxic effects that require careful evaluation. Gentisin can be used in vascular smooth muscle research. Specific in vivo efficacy data is limited in the available literature.
|
| Enzyme Assay |
In vitro enzyme assays for gentisin involve measuring its effects on enzymes involved in cell proliferation, oxidative stress, and inflammation. DNA synthesis inhibition is assessed by measuring BrdU incorporation in VSMC. Antioxidant activity is assessed using standard cell-free assays such as DPPH radical scavenging or ABTS. Anti-inflammatory activity can be evaluated by measuring inhibition of inflammatory enzymes. Antimicrobial activity is assessed using standard broth microdilution assays. These assays provide mechanistic insights into the compound's activities.
|
| Cell Assay |
In vitro cell-based assays for gentisin involve treating vascular smooth muscle cells with varying concentrations of the compound to assess its effects on cell proliferation and DNA synthesis. Cell proliferation is measured by cell counting or MTT assays. DNA synthesis is quantified by BrdU incorporation. Cell cycle analysis is performed by flow cytometry. Apoptosis is quantified using Annexin V/PI staining. The compound's effects on oxidative stress and inflammation can be assessed in appropriate cell types. These cellular studies characterize the compound's anti-proliferative activity.
|
| Animal Protocol |
In vivo animal experiments for gentisin have not been extensively reported. As a natural compound with anti-proliferative activity, it has potential applications in vascular smooth muscle research. Studies in animal models of vascular disease would be needed to assess in vivo efficacy. The compound's mutagenic activity suggests potential genotoxic effects that would require careful evaluation in vivo. Specific dosing regimens and detailed efficacy data are not available in the current literature.
|
| ADME/Pharmacokinetics |
Gentisin has a molecular formula of C14H10O5 and is a naturally occurring xanthone derivative. It is isolated from Gentiana lutea and other Gentianaceae species. The compound is typically extracted using organic solvents. Its solubility properties are characteristic of xanthone compounds. Specific pharmacokinetic data such as absorption, distribution, metabolism, and elimination are not extensively reported. The compound is typically stored under recommended conditions for natural products.
|
| Toxicity/Toxicokinetics |
Gentisin has mutagenic activity, indicating potential genotoxic effects. The compound's mutagenicity has been demonstrated in various assays. This property requires careful handling and consideration for any therapeutic applications. Despite its mutagenic activity, gentisin exhibits antioxidant, anti-inflammatory, and antimicrobial properties that may have beneficial effects. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound in research settings.
|
| References | |
| Additional Infomation |
Gentisin belongs to the xanthone class of compounds, with the structure 9H-xanthone-9-one, where hydroxyl groups are substituted at positions 1 and 7, and a methoxy group is substituted at position 3. It is a plant metabolite. Gentisin belongs to the xanthone, polyphenol, and aromatic ether class of compounds. It has been reported to be found in Polygala tenuifolia, Gentianopsis grandis, and other organisms with relevant data. See also: Leaf (part) of Menyanthes trifoliata.
Gentisin is a naturally occurring xanthone derivative (1,7-dihydroxy-3-methoxyxanthone) isolated from Gentiana lutea. It is a novel inhibitor of vascular smooth muscle cell proliferation with an IC50 of 7.84 μM. The compound has mutagenic activity and exhibits antioxidant, anti-inflammatory, and antimicrobial properties. Gentisin can be used in vascular smooth muscle research. It has potential applications in oxidative stress-related disorders. |
| Molecular Formula |
C14H10O5
|
|---|---|
| Molecular Weight |
258.229
|
| Exact Mass |
258.053
|
| CAS # |
437-50-3
|
| PubChem CID |
5281636
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.48g/cm3
|
| Boiling Point |
519.9ºC at 760mmHg
|
| Melting Point |
273 - 275 °C
|
| Flash Point |
205.2ºC
|
| Vapour Pressure |
1.99E-11mmHg at 25°C
|
| Index of Refraction |
1.68
|
| LogP |
2.366
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
19
|
| Complexity |
358
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
XOXYHGOIRWABTC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H10O5/c1-18-8-5-10(16)13-12(6-8)19-11-3-2-7(15)4-9(11)14(13)17/h2-6,15-16H,1H3
|
| Chemical Name |
1,7-dihydroxy-3-methoxyxanthen-9-one
|
| Synonyms |
BRN-0384788; BRN 0384788; Gentisin
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
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
|
|---|---|
| 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 | 3.8725 mL | 19.3626 mL | 38.7252 mL | |
| 5 mM | 0.7745 mL | 3.8725 mL | 7.7450 mL | |
| 10 mM | 0.3873 mL | 1.9363 mL | 3.8725 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
