Denatonium benzoate
Based on 2 publication(s) in Google Scholar
Denatonium benzoate (THS-839) is known as the most bitter compound and is commonly used as a deterrent (bittering agent) to activate different types of bitter taste receptors (TAS2Rs) with oral activity. Denatonium benzoate can enhance insulin secretion, has anti-inflammatory effects, and promotes allergy susceptibility .
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- Pureté : 99.87%
- CAS No.: 3734-33-6
- Formule: C28H34N2O3
- Masse moléculaire:446.58
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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HY-W011053
NeotameArtificial Sweetener -
HY-B1146R
Denatonium benzoate (Standard)Aversive Agent -
HY-100047
Nα,Nα-Bis(carboxymethyl)-L-lysineBitter taste receptors 4 Inhibitor -
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GIV3727Bitter Taste Receptor Antagonist -
HY-100047R
Nα,Nα-Bis(carboxymethyl)-L-lysine (Standard)Bitter taste receptors 4 Inhibitor -
HY-W011053GL
Neotame (GMP Like)Artificial Sweetener -
HY-W011053R
Neotame (Standard)Standard of Neotame
Publications Citing Use of MedChemExpress (MCE) Denatonium benzoate
More
Activité biologique
Description
IC50 & Target
TAS2Rs
In Vitro
Denatonium benzoate (15 μM, 5 min) reduces the spontaneous contraction activity of rat gastric smooth muscle strips[1].
Denatonium benzoate (10 μM, 24h) increases the release of β-hexosaminidase and the mobilization of Ca2+ in IgE-mediated activated RBL-2H3 and KU812 cells[2].
Denatonium benzoate (10 μM, 30 min) enhances the expression of FcεRIα on the surface of RBL-2H3 and KU812 cells[2].
Denatonium benzoate (0-25 mM, 24 h) inhibits the proliferation of RBL-2H3 and KU812 cells when above 0.1 mM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:RBL-2H3, KU812
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Concentration:0, 0.01, 0.05, 0.1, 0.5, 1, 2, 2.5, 4, 5, 10, 25 mM
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Incubation Time:24 h
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Result:Showed that 0.1 mM caused significant inhibition of cell viability in RBL-2H3 and KU812 cells in a dose-dependent manner.
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Cell Line:RBL-2H3, KU812
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Concentration:10 mM
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Incubation Time:30 min
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Result:Promoted the expression of FcεRIα on the surface of mast cells.
In Vivo
Denatonium benzoate (5 mg/kg, i.g., single dose) promotes allergy susceptibility in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat plantar edema model[1]
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Dosage:15 mg/kg, single dose
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced foot volume and had anti-inflammatory effects.
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Animal Model:BLAB/c mice induced by OVA[2]
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Dosage:5 mg/kg, every other day, 20 days
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Administration:i.g.
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Result:Caused more severe allergic reactions and promoted allergic susceptibility in mice. Acute diarrhea began after three to four intragastric stimulations, mucus accumulation in the jejunum, β-hex and histamine levels were significantly increased, and ova in serum Specific IgE levels are also elevated.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3734-33-6
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Appearance Solid
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Masse moléculaire 446.58
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Formule C28H34N2O3
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Color White to light yellow
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SMILES
CC[N+](CC)(CC(NC1=C(C)C=CC=C1C)=O)CC2=CC=CC=C2.O=C([O-])C3=CC=CC=C3
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Synonyms
THS-839
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Eur J Med Chem
2024 Dec 5:279:116842. PMID: 39260319
Solvant et solubilité
In Vitro:
H2O : 20 mg/mL (44.78 mM; Need ultrasonic)
DMSO : 20 mg/mL (44.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (74.63 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocole
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Human Islet Cell Culture
The method of preserving islets in vitro, with purified reduced immunogenicity. The steps are islet isolation, islet cell purification, in vitro determination of islet function and islet cell culture.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2392 mL | 11.1962 mL | 22.3924 mL | 55.9810 mL |
| 5 mM | 0.4478 mL | 2.2392 mL | 4.4785 mL | 11.1962 mL | |
| 10 mM | 0.2239 mL | 1.1196 mL | 2.2392 mL | 5.5981 mL | |
| 15 mM | 0.1493 mL | 0.7464 mL | 1.4928 mL | 3.7321 mL | |
| 20 mM | 0.1120 mL | 0.5598 mL | 1.1196 mL | 2.7991 mL | |
| 25 mM | 0.0896 mL | 0.4478 mL | 0.8957 mL | 2.2392 mL | |
| 30 mM | 0.0746 mL | 0.3732 mL | 0.7464 mL | 1.8660 mL | |
| 40 mM | 0.0560 mL | 0.2799 mL | 0.5598 mL | 1.3995 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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