Lactisole is a typical sweet taste receptor antagonist that selectively targets the T1R3 subunit. T1R3 is a glucose-sensing receptor. Lactisole inhibits glucose-induced insulin secretion from mouse islets.

Physicochemical Properties

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
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)

Biological Activity

Targets	T1R3[1]
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].
References	[1]. Lactisole inhibits the glucose-sensing receptor T1R3 expressed in mouse pancreatic β-cells. J Endocrinol. 2015 Jul;226(1):57-66. [2]. Sweet Taste Antagonist Lactisole Administered in Combination with Sucrose, But Not Glucose, Increases Energy Intake and Decreases Peripheral Serotonin in Male Subjects. Nutrients. 2020 Oct 14;12(10):3133.

Solubility Data

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. 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. 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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

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.