| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
The primary target of Ononetin is the TRPM3 (transient receptor potential melastatin 3) channel. It acts as a potent and selective blocker of TRPM3 with an IC50 of 0.3 µM. By blocking TRPM3, it modulates calcium influx and reduces pain and inflammation. Its selectivity for TRPM3 makes it a valuable tool for studying the role of this channel in pain pathways.
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| ln Vitro |
In primary cultures of mouse or rat dorsal root ganglia (DRG) neurones, ononetin (1–10 μM) completely and reversibly abolishes Ca2+ entry and ionic currents through recombinantly expressed TRPM3α2 and blocks the pregnenolone sulphate-inducible Ca2+ entry, indicating biological activity towards endogenously expressed TRPM3[1]. Ononetin's oxidative intermediates might be involved in activating TRPA1, but not in Ononetin's blocking of TRPM3[1].
In vitro, Ononetin is a potent and selective TRPM3 channel blocker with an IC50 of 0.3 µM. Its activity is typically measured using electrophysiological techniques (e.g., patch-clamp) or calcium imaging in cells expressing TRPM3 channels. Its selectivity for TRPM3 over other TRP channels is assessed. |
| ln Vivo |
Treatment with ononetin (10 mg/kg, ip) completely reverses heat hypersensitivity induced by Freund's Complete Adjuvant (FCA), indicating that TRPM3-/-mice's loss of hypersensitivity is unlikely to be due to compensatory or developmental mechanisms and pointing to TRPM3 as a potential target for inflammatory pain[2].
In vivo, Ononetin completely reverses heat hypersensitivity induced by Freund's Complete Adjuvant (FCA) in mice at a dose of 10 mg/kg (ip). This suggests that TRPM3 is a potential target for inflammatory pain. Its analgesic effects in animal models have been demonstrated. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Ononetin are not typically performed, as it is a channel blocker rather than a ligand for a specific receptor. Its activity is assessed in functional assays using cells expressing TRPM3 channels. Calcium influx or electrophysiological recordings are used to measure its blocking activity. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for Ononetin are conducted in cells expressing TRPM3 channels or in primary sensory neurons. Cells are treated with the compound, and calcium influx is measured using fluorescent indicators to assess TRPM3 activity. Its effects on neuronal excitability and pain signaling are assessed using electrophysiological techniques.
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| Animal Protocol |
In vivo animal studies for Ononetin are conducted in mouse models of inflammatory pain, such as the Freund's Complete Adjuvant (FCA)-induced heat hypersensitivity model. Animals are administered the compound intraperitoneally, and pain behavior (e.g., paw withdrawal latency) is assessed. Its effects on TRPM3-mediated pain are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Ononetin indicate it has a molecular weight of 258.27 and a molecular formula of C15H14O4. It is a natural deoxybenzoin. Its bioavailability and other PK parameters would be determined in preclinical studies. The compound is typically stored as a powder at appropriate conditions.
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| Toxicity/Toxicokinetics |
Toxicological information for Ononetin is limited to its use as a research chemical. As a TRPM3 channel blocker, it may have effects on pain and inflammation. Comprehensive toxicology studies would be required for clinical development, including assessments of its effects on neurological and cardiovascular function.
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| References |
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| Additional Infomation |
1-(2,4-Dihydroxyphenyl)-2-(4-methoxyphenyl)ethyl ketone is a stilbene compound.
Ononetin is a natural product and a potent and selective TRPM3 channel blocker. It is used to study the role of TRPM3 in pain and inflammation. It reverses heat hypersensitivity in animal models. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use. |
| Molecular Formula |
C15H14O4
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| Molecular Weight |
258.27
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| Exact Mass |
258.089
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| CAS # |
487-49-0
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| PubChem CID |
259632
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| Appearance |
White to off-white solid powder
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| Density |
1.275g/cm3
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| Boiling Point |
464.7ºC at 760mmHg
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| Melting Point |
158.0-162.0°C
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| Flash Point |
176.9ºC
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| Vapour Pressure |
2.95E-09mmHg at 25°C
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| Index of Refraction |
1.62
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| LogP |
2.531
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
297
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XHBZOAYMBBUURD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14O4/c1-19-12-5-2-10(3-6-12)8-14(17)13-7-4-11(16)9-15(13)18/h2-7,9,16,18H,8H2,1H3
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| Chemical Name |
1-(2,4-dihydroxyphenyl)-2-(4-methoxyphenyl)ethanone
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| Synonyms |
Ononetin1-(2,4-Dihydroxyphenyl)-2-(4-methoxyphenyl)ethanone
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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 (~387.19 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.68 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 (9.68 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 (9.68 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 | 3.8719 mL | 19.3596 mL | 38.7192 mL | |
| 5 mM | 0.7744 mL | 3.8719 mL | 7.7438 mL | |
| 10 mM | 0.3872 mL | 1.9360 mL | 3.8719 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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