| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Licogliflozin targets the sodium-glucose cotransporters SGLT1 and SGLT2. SGLT2 is primarily responsible for the reabsorption of glucose in the proximal tubule of the kidney, while SGLT1 is responsible for the remaining glucose reabsorption in the more distal segments of the nephron. By inhibiting both transporters, licogliflozin blocks almost all glucose reabsorption, leading to significant urinary glucose excretion and a reduction in blood glucose levels.
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| ln Vitro |
For the treatment of non-alcoholic steatohepatitis (NASH), licogliflozin (LIK066) is a non-antifibrotic medication.
In vitro, licogliflozin demonstrates potent inhibition of SGLT1 and SGLT2, with IC50 values of 22.0 nM against human SGLT1 and 0.5 nM against human SGLT2. This indicates that it is a highly potent inhibitor of both transporters, with a significantly higher potency for SGLT2. These in vitro activities confirm its mechanism as a dual SGLT1/2 inhibitor. |
| ln Vivo |
In vivo, licogliflozin is orally bioavailable. By inhibiting SGLT1 and SGLT2, it promotes urinary glucose excretion and lowers blood glucose levels. It is being investigated for the treatment of non-alcoholic steatohepatitis (NASH), suggesting that its effects extend beyond glucose control to potentially include metabolic benefits relevant to liver health.
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| Enzyme Assay |
Non-cell-based assays for licogliflozin typically involve measuring its ability to inhibit SGLT1 and SGLT2 activity in a cell-free system. This can be done using membrane preparations from cells expressing the transporters. The transporter is incubated with a radiolabeled glucose analog (e.g., [14C]-AMG) and licogliflozin at various concentrations. The amount of radiolabeled glucose taken up is measured, and an IC50 value is determined.
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| Cell Assay |
Cellular assays for licogliflozin are performed using cells that express human SGLT1 or SGLT2. The cells are incubated with a radiolabeled glucose analog and licogliflozin at various concentrations. The amount of radiolabeled glucose taken up by the cells is measured. The compound's ability to inhibit the uptake is quantified, and an IC50 value is determined.
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| Animal Protocol |
In vivo animal models for licogliflozin would typically involve the use of diabetic rodent models, such as db/db mice or streptozotocin-induced diabetic rats. The compound is administered orally, and its effect on urinary glucose excretion, blood glucose levels, and other metabolic parameters is measured. These studies are crucial for establishing the compound's in vivo efficacy.
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| ADME/Pharmacokinetics |
Licogliflozin has a molecular formula of C23H28O7. It is orally bioavailable. It is a small molecule that is likely to have good oral bioavailability. Detailed PK parameters such as half-life, Cmax, and bioavailability are not extensively detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for licogliflozin are not provided in the search results. As a dual SGLT1/2 inhibitor, its safety profile would be a key consideration. Potential side effects could include urinary tract infections, polyuria, and electrolyte imbalances. The compound is intended for research use only and is not for human consumption.
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| References | |
| Additional Infomation |
Linagliflozin is being investigated in the clinical trial NCT03320941 (a dose-exploratory study evaluating weight change after treatment with LIK066 in obese Japanese patients). Linagliflozin is an inhibitor of sodium-dependent glucose cotransporter (SGLT) family members 1 and 2 (SGLT1/2) with hypoglycemic activity. Linagliflozin inhibits glucose reabsorption in the proximal tubules of the kidney and promotes urinary glucose excretion by binding to and blocking SGLT1/2, thereby restoring normal blood glucose levels. SGLT1/2 is part of a transport system expressed in the proximal tubules that mediates the majority of glucose reabsorption from the tubular fluid by the kidneys.
Licogliflozin is also known as LIK-066. It is an orally bioavailable, potent dual inhibitor of SGLT1 and SGLT2. It has IC50 values of 22.0 nM against human SGLT1 and 0.5 nM against human SGLT2. It is being investigated for NASH and has the CAS number 1291094-73-9. It is supplied for research purposes. |
| Molecular Formula |
C23H28O7
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|---|---|
| Molecular Weight |
416.464227676392
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| Exact Mass |
416.183
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| CAS # |
1291094-73-9
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| Related CAS # |
1291095-45-8 (with proline);1291094-73-9;
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| PubChem CID |
52913524
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
546
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1[C@H](CO)[C@H]([C@@H]([C@H]([C@@H]1C1C=CC(CC)=C(CC2C=CC3=C(C=2)OCCO3)C=1)O)O)O
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| InChi Key |
XFJAMQQAAMJFGB-ZQGJOIPISA-N
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| InChi Code |
InChI=1S/C23H28O7/c1-2-14-4-5-15(23-22(27)21(26)20(25)19(12-24)30-23)11-16(14)9-13-3-6-17-18(10-13)29-8-7-28-17/h3-6,10-11,19-27H,2,7-9,12H2,1H3/t19-,20-,21+,22-,23+/m1/s1
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| Chemical Name |
(2S,3R,4R,5S,6R)-2-(3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
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| Synonyms |
LIK066 LIK-066 LIK 066 licogliflozin
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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 |
| 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 (~240.12 mM)
H2O : ~2 mg/mL (~4.80 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.00 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (24.01 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4012 mL | 12.0060 mL | 24.0119 mL | |
| 5 mM | 0.4802 mL | 2.4012 mL | 4.8024 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4012 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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