Lactisole (Synonyms: na-PMP) |
Catalog No.GC44024
One-Click Copy Product Info
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Lactisole is a canonical antagonist of sweet taste receptor, selectively targeting to T1R3 subunit.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 150436-68-3
Sample solution is provided at 25 µL, 10mM.
Lactisole is a canonical antagonist of sweet taste receptor, selectively targeting to T1R3 subunit[1]. 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, thereby triggering taste signaling pathways[2]. Lactisole blocks the activation of natural sweeteners by binding to the transmembrane domain of the receptor through a non-competitive allosteric mechanism and is commonly used in taste physiology and food science research[3-5].
In vitro, treatment of MIN6 cells with Lactisole(5-10mM; 1h) dose-dependently inhibits insulin secretion induced by sweeteners (acesulfame-K, sucralose, glycyrrhizin) and glucose (IC50=4mM), reduces intracellular [NADH] and [ATP] levels, attenuates Ca²⁺ elevation induced by these sweeteners and glucose, but does not affect cAMP elevation[6].
In vivo, co-administration of Lactisole (30mg/kg/day; i.g.; 12 weeks) and Alzheimer’s disease (AD) drug Sodium oligomannate (GV-971) attenuated the effects of GV-971 on serum serotonin and CCK levels, vagal afferent firing, and cognitive behaviors[7]. Oral administration of streptozotocin-induced diabetic male rats with Lactisole(10mg/kg; 2h) negates the beneficial effects of duodenal–jejunal bypass (DJB) surgeries on glucose tolerance by inhibiting GLP-1 and GLP-2 secretion, reducing intestinal villus height and crypt depth, and modulating the expression of taste receptors and glucose transporters[8].
References:
[1] Schiffman SS, Booth BJ, Sattely-Miller EA, Graham BG, Gibes KM. Selective inhibition of sweetness by the sodium salt of +/-2-(4-methoxyphenoxy)propanoic acid. Chem Senses. 1999;24(4):439-447.
[2] Kojima I, Nakagawa Y, Hamano K, Medina J, Li L, Nagasawa M. Glucose-Sensing Receptor T1R3: A New Signaling Receptor Activated by Glucose in Pancreatic β-Cells. Biol Pharm Bull. 2015;38(5):674-679.
[3] Jiang P, Cui M, Zhao B, et al. Lactisole interacts with the transmembrane domains of human T1R3 to inhibit sweet taste. J Biol Chem. 2005;280(15):15238-15246.
[4] Johnson C, Birch GG, MacDougall DB. The effect of the sweetness inhibitor 2(-4-methoxyphenoxy)propanoic acid (sodium salt) (Na-PMP) on the taste of bitter-sweet stimuli. Chem Senses. 1994;19(4):349-358.
[5] Schweiger K, Grüneis V, Treml J, et al. Sweet Taste Antagonist Lactisole Administered in Combination with Sucrose, But Not Glucose, Increases Energy Intake and Decreases Peripheral Serotonin in Male Subjects. Nutrients. 2020;12(10):3133.
[6] Hamano K, Nakagawa Y, Ohtsu Y, et al. Lactisole inhibits the glucose-sensing receptor T1R3 expressed in mouse pancreatic β-cells. J Endocrinol. 2015;226(1):57-66.
[7] Gong HS, Pan JP, Guo F, et al. Sodium oligomannate activates the enteroendocrine-vagal afferent pathways in APP/PS1 mice. Acta Pharmacol Sin. 2024;45(9):1821-1831.
[8] Sun S, Wang A, Kou R, et al. Duodenal-Jejunal Bypass Restores Sweet Taste Receptor-Mediated Glucose Sensing and Absorption in Diabetic Rats. J Diabetes Res. 2024;2024:5544296.
| Cell experiment [1]: | |
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Cell lines |
MIN6 cells |
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Preparation Method |
MIN6 cells were cultured in a 24-well plate and incubated for 48h. Cells were then incubated for 1h in KRH buffer containing 136mmol/l NaCl, 4.8mmol/l KCl, 1.3mmol/l CaCl2, 1.2mmol/l MgSO4, 1.2mmol/l KH2PO4, 5.0mmol/l NaHCO3, 10mmol/l HEPES/NaOH (pH 7.4) and 0.1% BSA. Cells were then incubated for 1h in the same buffer containing 5.5mmol/l glucose in the presence and absence of sweeteners (acesulfame-K, sucralose, glycyrrhizin) and Lactisole(5-10mM). The supernatant was collected and centrifuged at 300g for 10min to remove cell debris. The insulin concentration in the supernatant was measured by RIA according to the manufacturer’s protocol. Statistical analysis was performed by using Student’s t-test. |
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Reaction Conditions |
5-10mM; 1h |
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Applications |
Lactisole(5-10mM; 1h) dose-dependently inhibits insulin secretion induced by sweeteners (acesulfame-K, sucralose, glycyrrhizin) and glucose. |
| Animal experiment [2]: | |
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Animal models |
APP/PS1 mice |
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Preparation Method |
APP/PS1 mice were randomly divided into 4 groups (n = 6–7/group), namely Vehicle, GV-971, GV-971+Lactisole, and Lactisole, and gavaged with water, GV-971 (100mg/kg/day) and/or Lactisole (30mg/kg/day) for 12 weeks starting at 7 months. After completion of behavior tests, animals were euthanized and tissues samples (blood and jejunum) were collected for analysis. |
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Dosage form |
30mg/kg/day; i.g.; 12 weeks |
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Applications |
Co-administration of Lactisole (30mg/kg/day; i.g.; 12 weeks) and Alzheimer’s disease (AD) drug Sodium oligomannate (GV-971) attenuated the effects of GV-971 on serum serotonin and CCK levels, vagal afferent firing, and cognitive behaviors. |
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References: |
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| Cas No. | 150436-68-3 | SDF | |
| Synonyms | na-PMP | ||
| Chemical Name | 2-(4-methoxyphenoxy)-propanoic acid, monosodium salt | ||
| Canonical SMILES | COC1=CC=C(OC(C)C([O-])=O)C=C1.[Na+] | ||
| Formula | C10H11O4•Na | M.Wt | 218.2 |
| Solubility | 10mg/mL in DMSO,20mg/mL in DMF, 1mg/mL in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.583 mL | 22.9148 mL | 45.8295 mL |
| 5 mM | 916.6 μL | 4.583 mL | 9.1659 mL |
| 10 mM | 458.3 μL | 2.2915 mL | 4.583 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)