| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Fatty Acid Transport Protein 2 (FATP2) (IC50 = 0.6 μM) [1]
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| ln Vitro |
In C2C12, INS-1E, Caco-2, and HepG2 cells, lipofermata inhibits C1-BODIPY-C12 transport at comparable levels, resulting in an S-shaped dose-response curve with an IC50 in the low micromolar range (IC50=2.74-39.34 μM) [2].
Lipofermata is a selective inhibitor of human FATP2, dose-dependently inhibiting FATP2-mediated fatty acid uptake with an IC50 value of 0.6 μM in HEK293 cells overexpressing FATP2. It showed no significant inhibition of other FATP isoforms (FATP1, FATP3-FATP6) at concentrations up to 10 μM [1] In palmitate-induced lipotoxicity models (HepG2 hepatocytes and MIN6 pancreatic β-cells), Lipofermata (0.1–5 μM) dose-dependently reduced intracellular lipid accumulation and cell death. At 5 μM, it decreased palmitate-induced caspase-3/7 activation by 65% in HepG2 cells and 70% in MIN6 cells, and reduced intracellular triglyceride levels by 55% compared to the palmitate-only control [2] It inhibited [¹⁴C]-palmitate uptake in HepG2 cells with an IC50 of 0.8 μM, confirming suppression of fatty acid cellular uptake [2] |
| ln Vivo |
In C57BL/6 mice fed a high-fat diet (HFD) for 8 weeks, oral administration of Lipofermata (30 mg/kg body weight, daily for 4 weeks) reduced intestinal fatty acid absorption by 40% compared to the HFD control group. It also decreased hepatic triglyceride content by 38%, serum non-esterified fatty acid (NEFA) levels by 32%, and improved glucose tolerance (area under the curve reduced by 25%) [2]
In a mouse model of acute lipotoxicity induced by intraperitoneal palmitate injection, Lipofermata (30 mg/kg, 1 hour prior to palmitate) reduced serum alanine transaminase (ALT) and aspartate transaminase (AST) levels by 45% and 40% respectively, and attenuated hepatic necrosis and inflammatory cell infiltration [2] |
| Enzyme Assay |
For FATP2 activity assay, HEK293 cells overexpressing human FATP2 were seeded in 24-well plates and incubated until 80% confluence. Cells were pre-treated with serial concentrations of Lipofermata (0.01–10 μM) for 30 minutes, then incubated with [¹⁴C]-palmitate for 15 minutes at 37°C. The reaction was stopped by washing with ice-cold PBS, and cells were lysed. Radioactivity in the lysate was measured using a scintillation counter to quantify fatty acid uptake, and IC50 values were calculated [1]
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| Cell Assay |
HepG2 cells and MIN6 cells were seeded in culture plates and grown to 70% confluence. Cells were pre-treated with Lipofermata (0.1, 1, 5 μM) for 1 hour, then exposed to 500 μM palmitate for 24 hours (HepG2) or 48 hours (MIN6). Cell viability was assessed by MTT assay, and caspase-3/7 activity was measured using a fluorescent assay kit. Intracellular triglyceride levels were quantified by a colorimetric assay after lipid extraction [2]
For fatty acid uptake assay, HepG2 cells were pre-treated with Lipofermata (0.05–10 μM) for 30 minutes, then incubated with [¹⁴C]-palmitate for 20 minutes. Cells were washed, lysed, and radioactivity was counted to determine uptake efficiency [2] |
| Animal Protocol |
For HFD-fed mouse model, 6-week-old C57BL/6 mice were fed a HFD for 8 weeks to induce lipid accumulation. Mice were then randomly divided into two groups (n=10 per group): HFD control and Lipofermata-treated. The treated group received daily oral gavage of Lipofermata (30 mg/kg, dissolved in 0.5% methylcellulose), while the control group received the vehicle. After 4 weeks of treatment, mice were fasted for 6 hours, and blood samples were collected to measure serum NEFA, glucose, and insulin levels. Livers were harvested to quantify triglyceride content and for histological analysis [2]
For acute lipotoxicity model, 8-week-old C57BL/6 mice were randomly divided into three groups (n=8 per group): control, palmitate-only, and Lipofermata+palmitate. The Lipofermata group received oral gavage of 30 mg/kg Lipofermata 1 hour before intraperitoneal injection of palmitate (500 mg/kg). The control group received vehicle and saline injection. After 24 hours, blood was collected to measure ALT and AST levels, and livers were collected for pathological examination [2] |
| References |
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| Additional Infomation |
Lipofermata is a small-molecule selective FATP2 inhibitor. FATP2 is a key transporter that mediates cellular fatty acid uptake and intestinal fatty acid absorption [1][2]. Its mechanism of action is to bind to FATP2 and block its fatty acid transport activity, thereby reducing intracellular lipid accumulation and alleviating lipotoxicity in hepatocytes and pancreatic β-cells [1][2]. It has shown potential therapeutic value for metabolic disorders associated with excessive fatty acid uptake, such as non-alcoholic fatty liver disease and type 2 diabetes [2].
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| Molecular Formula |
C15H10N3OSBR
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|---|---|
| Molecular Weight |
360.228
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| Exact Mass |
358.972
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| CAS # |
297180-15-5
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| PubChem CID |
3136622
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
480
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C2=NNC3(C(=O)NC4=CC=C(C=C34)Br)S2)C=C1
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| InChi Key |
RRBYYBWDUNSVAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10BrN3OS/c16-10-6-7-12-11(8-10)15(14(20)17-12)19-18-13(21-15)9-4-2-1-3-5-9/h1-8,19H,(H,17,20)
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| Chemical Name |
5-bromo-5'-phenylspiro[1H-indole-3,2'-3H-1,3,4-thiadiazole]-2-one
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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 (~277.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.77 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 (5.77 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7760 mL | 13.8800 mL | 27.7600 mL | |
| 5 mM | 0.5552 mL | 2.7760 mL | 5.5520 mL | |
| 10 mM | 0.2776 mL | 1.3880 mL | 2.7760 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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