| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| 5g | |||
| Other Sizes |
| Targets |
Sofalcone acts as a gastric mucosal protective agent by increasing gastric mucosal blood flow and promoting mucosal repair. It inhibits prostaglandin-degrading enzymes, such as 5-hydroxyprostaglandin dehydrogenase, thereby increasing gastric prostaglandin levels. It also induces the expression of heme oxygenase-1 (HO-1), which has cytoprotective and anti-inflammatory effects.
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| ln Vitro |
Sofacone (50 μmol/L) dramatically raised the expression of HO-1 mRNA in trophoblast and HUVEC in comparison to the control group (both P<0.05). Sofalcone was able to significantly raise the expression of HO-1 protein in primary HUVEC that had been treated for 24 hours, according to Western blot analysis. Additionally, a 6-hour treatment with sofalcone (50 μmol/L) resulted in a considerable increase in Nrf2 content in the nuclear fraction of HUVEC, as demonstrated by Western blot analysis. Following a 24-hour treatment with sofacone, NQO1, TXN, and GCLC expression rose in primary HUVEC in a dose-dependent manner. Sofalcone decreases THP-1 monocyte adhesion to HUVEC in a dose-dependent manner and dramatically lowers the concentration of sFlt-1 in the culture media [1].
In vitro, Sofalcone induces the expression of Heme oxygenase-1 (HO-1) in gastric epithelium. It exhibits anti-inflammatory and antioxidant activities. Its effects on HO-1 induction and prostaglandin levels can be studied in gastric epithelial cell lines. |
| ln Vivo |
In vivo, Sofalcone increases gastric mucosal blood flow, dilates gastric mucosal blood vessels, and increases gastric tissue oxygen consumption. It promotes the repair of the gastric mucosa and increases the levels of prostaglandins within the stomach. It is effective against gastric ulcers.
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| Enzyme Assay |
In vitro enzyme assays for Sofalcone typically involve measuring the inhibition of prostaglandin-degrading enzymes, such as 5-hydroxyprostaglandin dehydrogenase. The compound's ability to induce heme oxygenase-1 (HO-1) expression can also be assessed in gastric epithelial cell lines using Western blotting or qPCR.
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| Cell Assay |
In vitro cellular assays for Sofalcone involve treating gastric epithelial cells with the compound and measuring its effects on HO-1 expression, prostaglandin levels, and cell viability. The compound's cytoprotective effects against oxidative stress or other insults can also be assessed in these assays.
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| Animal Protocol |
In vivo animal models for Sofalcone typically involve rat models of gastric ulcer induced by various agents (e.g., ethanol, stress, or non-steroidal anti-inflammatory drugs). The compound is administered orally, and its effects on ulcer healing, gastric mucosal blood flow, and prostaglandin levels are assessed.
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| ADME/Pharmacokinetics |
Sofalcone has a molecular formula of C27H30O6 and a molecular weight of 450.52 g/mol. Its IUPAC name is 2-(5-((3-Methylbut-2-en-1-yl)oxy)-2-(3-(4-((3-methylbut-2-en-1-yl)oxy)phenyl)acryloyl)phenoxy)acetic acid. It is a stable synthetic analog of sophoradin. The compound is for research use only.
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| Toxicity/Toxicokinetics |
Sofalcone is a gastric antiulcer agent with a well-characterized mechanism of action. Its safety profile has been established in preclinical and clinical studies. As with any drug, it may have potential side effects. The compound is for research use only and is not approved for human therapeutic use in many regions.
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| References | |
| Additional Infomation |
Sofalcone is a chalcone compound with a benzene structure, wherein the hydrogen atoms at positions 1, 2, and 5 are substituted with carboxymethoxy, (1E)-1-{4-[(3-methylbut-2-en-1-yl)oxy]phenyl}-3-oxopropyl-1-en-3-yl, and (3-methylbut-2-en-1-yl)oxy, respectively. It is a gastrointestinal drug currently used in Japan and South Korea to treat gastritis and gastric ulcers. It possesses multiple functions, including anti-ulcer agent, gastrointestinal drug, plant metabolite, and antibacterial agent. It is an aromatic ether, a monocarboxylic acid, and belongs to the chalcone class of compounds. Sofalcone has been reported as a mucosal protectant that inhibits the growth of Helicobacter pylori. It inhibits the adhesion of Helicobacter pylori, the production of vacuolating toxin (VT), and the secretion of interleukin-8 (IL-8). [Drug Indications] It has been studied for the treatment of gastroenteritis and ulcers.
Mechanism of Action According to reports, sofadone has antibacterial activity against Helicobacter pylori and can inhibit the pathogenic factors of Helicobacter pylori. It also has a mucosal protective effect due to the inhibition of prostaglandin-degrading enzymes. Sofadone has a direct bactericidal effect against Helicobacter pylori, exhibits anti-urease activity, and can reduce the adhesion of the bacteria to gastric epithelial cells. Sofalcone (CAS# 64506-49-6) is a synthetic analog of sophoradin and a gastric antiulcer agent. It induces heme oxygenase-1 (HO-1) expression, increases gastric mucosal blood flow, and inhibits prostaglandin degradation. The compound has anti-inflammatory and antioxidant activities and is for research use only. |
| Molecular Formula |
C27H30O6
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|---|---|
| Molecular Weight |
450.53
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| Exact Mass |
450.204
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| CAS # |
64506-49-6
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| PubChem CID |
5282219
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
650.0±55.0 °C at 760 mmHg
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| Flash Point |
215.2±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.579
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| LogP |
6.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
33
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| Complexity |
706
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=CCOC1=CC=C(C=C1)/C=C/C(=O)C2=C(C=C(C=C2)OCC=C(C)C)OCC(=O)O)C
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| InChi Key |
GFWRVVCDTLRWPK-KPKJPENVSA-N
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| InChi Code |
InChI=1S/C27H30O6/c1-19(2)13-15-31-22-8-5-21(6-9-22)7-12-25(28)24-11-10-23(32-16-14-20(3)4)17-26(24)33-18-27(29)30/h5-14,17H,15-16,18H2,1-4H3,(H,29,30)/b12-7+
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| Chemical Name |
2-[5-(3-methylbut-2-enoxy)-2-[(E)-3-[4-(3-methylbut-2-enoxy)phenyl]prop-2-enoyl]phenoxy]acetic acid
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| Synonyms |
Isoprenyl chalcone; BRN 2191482; Sofalcone
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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 : ≥ 100 mg/mL (~221.97 mM)
H2O : ~0.67 mg/mL (~1.49 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2196 mL | 11.0980 mL | 22.1961 mL | |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2196 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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