| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
T1R3[1]
Lactisole targets the sweet taste receptor, specifically the T1R3 subunit. T1R3 is a common key subunit of the sweet taste receptor (hT1R2/hT1R3) and the umami taste receptor (hT1R1/hT1R3), responsible for recognizing sugars, artificial sweeteners and L-amino acids. By binding to T1R3, lactisole acts as an antagonist and blocks the activation of the sweet taste receptor by sweet compounds. This reduces both sweetness intensity and persistence. |
|---|---|
| ln Vitro |
In mouse pancreatic β-cell MIN6 (IC50~4 mM), lactisole (3-10 mM; 48 h) suppresses insulin secretion produced by acesulfame-K, sucrose, and glycophorin [1]. Without altering the rise in intracellular cAMP concentration ([cAMP]c), lactisole (5 mM; 48 h) reduces the increase in cytoplasmic Ca2+ concentration ([Ca2+]c) brought on by sucrose and acesulfame-K [1].
In vitro, lactisole inhibits glucose-induced insulin secretion from mouse islets. In MIN6 cells (a mouse pancreatic β-cell line), lactisole suppresses insulin secretion produced by sweeteners such as acesulfame-K, sucralose, and glycyrrhizin in a dose-dependent manner, with an IC₅₀ of approximately 4 mM. Lactisole (5 mM) reduces the increase in cytoplasmic Ca²⁺ concentration brought on by sucrose and acesulfame-K without altering the rise in intracellular cAMP concentration. |
| ln Vivo |
In vivo, lactisole has been studied for its effects on glucose metabolism and insulin secretion. By inhibiting the sweet taste receptor, it can modulate glucose-sensing mechanisms in the body. However, detailed in vivo activity data for lactisole are not extensively reported in the search results. Its primary application is as a research tool to study sweet taste perception and glucose-sensing pathways.
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| Enzyme Assay |
Non-cellular assays for lactisole involve studying its binding to the T1R3 sweet taste receptor. This can be assessed using techniques such as surface plasmon resonance (SPR) or radioligand binding assays. The compound's ability to inhibit the activation of the receptor by sweet ligands can be measured in cell-free systems.
|
| Cell Assay |
Cell-based assays for lactisole involve studying its effects on sweet taste receptor signaling in cells expressing T1R3. Cells can be treated with sweet compounds in the presence or absence of lactisole, and receptor activation can be measured using calcium imaging or reporter gene assays. The compound's effects on insulin secretion can be studied in MIN6 cells or pancreatic islets.
|
| Animal Protocol |
In vivo animal experiments with lactisole have been conducted to study its effects on taste perception and glucose metabolism. In rodents, the compound has been used to investigate the role of sweet taste receptors in the gut and pancreas. However, lactisole does not inhibit sweetness perception in rats, limiting its use in some animal models.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for lactisole have not been extensively reported. The compound is soluble in DMSO at 125 mg/mL. It can be formulated for in vivo use in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline at ≥2.08 mg/mL.
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| Toxicity/Toxicokinetics |
No specific toxicity data have been reported for lactisole. As a food-derived compound, it is generally considered to have a favorable safety profile.
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| References |
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| Additional Infomation |
Lactisole is a research compound, not an approved drug. It is a typical sweet taste receptor antagonist that selectively targets the T1R3 subunit. It is used as a tool to study sweet taste perception and glucose-sensing mechanisms. The compound is not intended for human therapeutic use.
|
| Molecular Formula |
C10H11NAO4
|
|---|---|
| Molecular Weight |
218.18
|
| Exact Mass |
196.073
|
| CAS # |
150436-68-3
|
| PubChem CID |
23670520
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
331.6±17.0 °C at 760 mmHg
|
| Flash Point |
130.3±14.4 °C
|
| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
| Index of Refraction |
1.521
|
| LogP |
1.65
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
15
|
| Complexity |
190
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C(=O)[O-])OC1=CC=C(C=C1)OC.[Na+]
|
| InChi Key |
SKORRGYRKQDXRS-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C10H12O4.Na/c1-7(10(11)12)14-9-5-3-8(13-2)4-6-9;/h3-7H,1-2H3,(H,11,12);/q;+1/p-1
|
| Chemical Name |
sodium;2-(4-methoxyphenoxy)propanoate
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 125 mg/mL (572.92 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.53 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 20.8 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: ≥ 2.08 mg/mL (9.53 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 20.8 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: ≥ 2.08 mg/mL (9.53 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 | 4.5834 mL | 22.9169 mL | 45.8337 mL | |
| 5 mM | 0.9167 mL | 4.5834 mL | 9.1667 mL | |
| 10 mM | 0.4583 mL | 2.2917 mL | 4.5834 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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