| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Intestinal smooth muscle and mucosal cells. Oxyphenisatine acts as a stimulant laxative by increasing intestinal motility and fluid secretion in the colon. The compound may stimulate the myenteric plexus and alter electrolyte transport in the intestinal mucosa. Its mechanism of action is similar to other diphenylmethane laxatives such as bisacodyl and phenolphthalein.
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| ln Vitro |
It has been demonstrated that oxifen possesses antiproliferative properties. Orfenisadine acetate's prodrug is orbenisadine acetate (OXY, NSC 59687). The growth of T47D, MCF7, HS578T, and MDA-MB-468 breast cancer cell lines is inhibited by OXY (IC50=0.8, 0.6, 2.1, 1.8 μM). This phenomenon is linked to specific suppression of translation and is accompanied by fast phosphorylation of GCN2, PERK, and the nutrient-sensing eIF2α kinase [1].
Oxyphenisatine stimulates intestinal motility and increases fluid secretion in the colon in vitro. Studies have shown that the compound increases peristaltic activity in isolated intestinal preparations. The compound also affects electrolyte transport in intestinal mucosal cells, leading to increased fluid accumulation in the intestinal lumen. Its effects are dose-dependent. |
| ln Vivo |
Mice may withstand intraperitoneal injections of OXY at doses of 300 mg/kg once day or 200 mg/kg twice daily, according to research on toxicity. The tumor size dramatically decreased from day 33 to day 52 following an intraperitoneal injection of OXY at a dose of 300 mg/kg once day for ten days [1].
Oxyphenisatine has been used as a stimulant laxative in clinical practice. The compound is effective in relieving constipation by stimulating intestinal motility and increasing fluid secretion. However, its use has been limited due to concerns about hepatotoxicity. The compound has been associated with cases of liver injury and has been withdrawn from the market in some countries. |
| Enzyme Assay |
In vitro assays for Oxyphenisatine include studies on intestinal smooth muscle contraction and electrolyte transport. Isolated intestinal segments are used to measure peristaltic activity and contractile responses to the compound. Ussing chamber studies are used to assess the effects on ion transport across intestinal mucosal preparations. Receptor binding studies may be performed to identify the molecular targets.
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| Cell Assay |
Cellular assays for Oxyphenisatine are performed using intestinal epithelial cell lines (e.g., Caco-2, T84) to study its effects on electrolyte transport and barrier function. Cells are treated with the compound, and transepithelial electrical resistance (TEER) and ion flux are measured. Cell viability is assessed to evaluate cytotoxicity. The compound's effects on intracellular signaling pathways are studied using Western blot or other molecular techniques.
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| Animal Protocol |
In vivo animal studies for Oxyphenisatine are performed in rodent models to assess laxative activity and toxicity. Animals are administered the compound orally, and gastrointestinal transit time, fecal output, and water content are measured. Toxicity studies assess liver function and histopathology. The compound has been associated with hepatotoxicity in animal models, which has limited its clinical use.
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| ADME/Pharmacokinetics |
Oxyphenisatine has a molecular weight of 349.34 g/mol and molecular formula C20H15NO5. It is a crystalline solid with low aqueous solubility. The compound should be stored under standard laboratory conditions. For in vitro studies, it is typically dissolved in DMSO or other organic solvents. The compound is light-sensitive and should be protected from light.
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| Toxicity/Toxicokinetics |
Oxyphenisatine has been associated with hepatotoxicity, including cases of acute liver injury and chronic liver disease. The compound has been withdrawn from the market in some countries due to safety concerns. Standard laboratory safety precautions should be followed when handling the compound. The compound is for research use only and is not for human therapeutic use.
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| References | |
| Additional Infomation |
Propofol belongs to the indole class of drugs. It is an enterohepatic laxative and may cause jaundice.
Oxyphenisatine (oxyphenisatin) is a stimulant laxative that has been used for the treatment of constipation. It acts by stimulating intestinal motility and increasing fluid secretion in the colon. However, the compound has been associated with hepatotoxicity and has been withdrawn from the market in some countries. Oxyphenisatine is a derivative of phenolphthalein and has similar pharmacological properties. The compound is for research use only and is not for clinical use. It serves as a tool for studying intestinal motility and laxative mechanisms. |
| Molecular Formula |
C20H15NO3
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|---|---|
| Molecular Weight |
317.34
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| Exact Mass |
317.105
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| CAS # |
125-13-3
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| Related CAS # |
Oxyphenisatin acetate;115-33-3
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| PubChem CID |
31315
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| Appearance |
White to off-white solid powder
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| Density |
1.352g/cm3
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| Boiling Point |
562.9ºC at 760 mmHg
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| Flash Point |
294.2ºC
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| Vapour Pressure |
2.82E-13mmHg at 25°C
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| Index of Refraction |
1.691
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| LogP |
3.522
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SJDACOMXKWHBOW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15NO3/c22-15-9-5-13(6-10-15)20(14-7-11-16(23)12-8-14)17-3-1-2-4-18(17)21-19(20)24/h1-12,22-23H,(H,21,24)
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| Chemical Name |
3,3-bis(4-hydroxyphenyl)-1H-indol-2-one
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| Synonyms |
Diphenolisatin; Critex; Oxyphenisatine
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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 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~787.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1512 mL | 15.7560 mL | 31.5119 mL | |
| 5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL | |
| 10 mM | 0.3151 mL | 1.5756 mL | 3.1512 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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