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| 5mg |
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| 50mg |
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| Targets |
The primary target of o-3M3FBS is phospholipase C (PLC). It acts as a potent and irreversible activator of PLC. PLC is a key enzyme involved in cell signaling and is activated by various cell surface receptors, including G-protein coupled receptors and receptor tyrosine kinases. By activating PLC, o-3M3FBS stimulates the production of inositol trisphosphate (IP3) and diacylglycerol (DAG), leading to calcium release and activation of protein kinase C (PKC).
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| ln Vitro |
In vitro, o-3M3FBS stimulates cytoplasmic calcium increase, inositol phosphate formation, and superoxide generation in human cells. It is a potent activator of PLC, and its effects can be blocked by the PLC inhibitor U-73122. It is used to study PLC signaling in various cell types. Its activity is typically measured by monitoring calcium flux using fluorescent indicators or by measuring inositol phosphate accumulation.
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| ln Vivo |
o-3M3FBS (10 μM) decreased the AUC to 840±134 g/min from 1058±189 g/min in the control (with TTX present). Increased o-3M3FBS concentrations (25 μM) further decreased the AUC to 457±59 g/min[1].
In vivo, o-3M3FBS is used to study PLC signaling in animals in conjunction with the PLC inhibitor U-73122. Specific in vivo study protocols are not extensively detailed in the available literature, but it is used as a pharmacological tool to modulate PLC activity in vivo. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for o-3M3FBS are not typically performed, as it is an activator of PLC rather than a ligand for a specific receptor. Its activity is assessed in functional assays using purified PLC enzyme or cell lysates. PLC activity is measured by monitoring the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) to IP3 and DAG. The compound's ability to activate PLC is determined by measuring the increase in enzymatic activity.
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| Cell Assay |
In vitro cellular assays for o-3M3FBS are conducted in various cell lines. Cells are treated with the compound, and PLC activation is assessed by measuring IP3 production, calcium mobilization using fluorescent dyes (e.g., Fura-2 or Fluo-4), or DAG production. Superoxide generation can be measured using chemiluminescent or colorimetric assays. The PLC inhibitor U-73122 is used as a control to confirm the specificity of the effects.
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| Animal Protocol |
In vivo animal studies for o-3M3FBS are not extensively documented. As a research tool, it may be administered to animals to study the role of PLC in various physiological and pathological processes. Its effects on PLC signaling in vivo can be assessed by measuring downstream signaling molecules or physiological responses. The PLC inhibitor U-73122 can be used as a control to confirm the specificity of the effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of o-3M3FBS indicate it has a molecular weight of 343.36 and a molecular formula of C16H16F3NO2S. It is soluble in DMSO at 100 mg/mL. The compound is typically stored at room temperature. Its bioavailability and other PK parameters would be determined in preclinical studies for its use as a research tool.
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| Toxicity/Toxicokinetics |
Toxicological information for o-3M3FBS is limited to its use as a research chemical. As a PLC activator, it may have effects on various cellular processes, including cell growth, differentiation, and motility. Comprehensive toxicology studies would be required for its use in vivo, including assessments of its effects on calcium homeostasis and cell signaling.
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| References |
[1]. Dwyer L, et al. Phospholipase C-independent effects of 3M3FBS in murine colon. Eur J Pharmacol. 2010;628(1-3):187-194.
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| Additional Infomation |
2,4,6-Trimethyl-N-[2-(trifluoromethyl)phenyl]benzenesulfonamide is a sulfonamide.
o-3M3FBS is a research compound used as a potent and irreversible activator of phospholipase C (PLC). It is also known as 2,4,6-trimethyl-N-[2-(trifluoromethyl)phenyl]benzenesulfonamide. It is used in conjunction with the PLC inhibitor U-73122 to study PLC signaling in cells and animals. It is not approved for clinical use and is available from research chemical suppliers. |
| Molecular Formula |
C16H16F3NO2S
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|---|---|
| Molecular Weight |
343.36
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| Exact Mass |
343.085
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| CAS # |
313981-55-4
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| PubChem CID |
770820
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| Appearance |
White to off-white solid powder
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| Density |
1.316g/cm3
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| Boiling Point |
424.3ºC at 760mmHg
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| Flash Point |
210.4ºC
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| Index of Refraction |
1.547
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| LogP |
5.585
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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 |
3
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| Heavy Atom Count |
23
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C(=C1)C)S(=O)(=O)NC2=CC=CC=C2C(F)(F)F)C
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| InChi Key |
SKJJIFRWCCSXGL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16F3NO2S/c1-10-8-11(2)15(12(3)9-10)23(21,22)20-14-7-5-4-6-13(14)16(17,18)19/h4-9,20H,1-3H3
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| Chemical Name |
2,4,6-trimethyl-N-[2-(trifluoromethyl)phenyl]benzenesulfonamide
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| Synonyms |
o3M3FBS; o 3M3FBS; o-3M3FBS
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~291.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.28 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 (7.28 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9124 mL | 14.5620 mL | 29.1240 mL | |
| 5 mM | 0.5825 mL | 2.9124 mL | 5.8248 mL | |
| 10 mM | 0.2912 mL | 1.4562 mL | 2.9124 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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