| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
FATP1-IN-1 targets fatty acid transport protein 1 (FATP1/SLC27A1), a bifunctional protein that facilitates the transport of long-chain fatty acids across the plasma membrane and catalyzes their conversion to acyl-CoA esters. By inhibiting FATP1, the compound blocks both the uptake and activation of long-chain fatty acids in cells, making it a valuable chemical probe for investigating the role of FATP1 in various metabolic pathways.
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| ln Vitro |
In vitro, FATP1-IN-1 potently inhibits the acyl-CoA synthetase activity of recombinant human FATP1 with an IC₅₀ value of 0.046 μM. For recombinant mouse FATP1, the IC₅₀ value is 0.60 μM. This potent inhibition is essential for blocking FATP1 function and modulating fatty acid metabolism in cells.
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| ln Vivo |
The results of the FATP1-IN-1 (po; 10 mg/kg) therapy indicate that it surpasses the mouse IC50 value of 0.22 μM without taking plasma protein binding into account. The Cmax, AUC, and Tmax were 5.5 μg/mL, 36 μg h/mL, and 0.33 hours, respectively.
In vivo, FATP1-IN-1 has demonstrated favorable pharmacokinetic properties in animal models. In one study, oral administration (p.o.) at 10 mg/kg showed a Cmax of 5.5 μg/mL, an AUC of 36 μg h/mL, and a Tmax of 0.33 hours, exceeding the mouse IC₅₀ value of 0.22 μM. By inhibiting FATP1, the compound can affect fatty acid uptake and oxidation in tissues such as adipose tissue, muscle, and liver, making it a potential tool for studying metabolic diseases. |
| Enzyme Assay |
Non-cellular assays for FATP1-IN-1 involve measuring its inhibitory activity against the acyl-CoA synthetase function of FATP1. This is typically done using recombinant human or mouse FATP1 protein in an enzymatic assay that measures the conversion of fatty acids to acyl-CoA in the presence of ATP and CoA. The inhibition of this activity is used to determine the IC₅₀ value.
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| Cell Assay |
Cell-based assays for FATP1-IN-1 involve measuring its effects on fatty acid uptake and metabolism in cells expressing FATP1. Cells can be treated with the compound, and the uptake of fluorescently labeled or radiolabeled fatty acids can be measured. Additionally, the effects on cellular lipid accumulation, fatty acid oxidation, and downstream signaling pathways can be assessed.
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| Animal Protocol |
Animal/Disease Models: Mouse plasma[1]
Doses: 10 mg/kg Route of Administration: Po Experimental Results: The Cmax, AUC and Tmax were 5.5 μg/mL, 36 μg h/mL and 0.33 hrs (hours), respectively. In vivo animal experiments with FATP1-IN-1 would typically involve administering the compound to mice or rats to study its effects on systemic fatty acid metabolism. Animal models of obesity, diabetes, or non-alcoholic fatty liver disease (NAFLD) could be used. Parameters such as body weight, food intake, glucose tolerance, insulin sensitivity, and tissue lipid content would be measured. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for FATP1-IN-1 show favorable properties. Following oral administration at 10 mg/kg, the compound achieved a Cmax of 5.5 μg/mL, an AUC of 36 μg h/mL, and a Tmax of 0.33 hours. The compound is soluble in DMSO at 62.5 mg/mL.
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| Toxicity/Toxicokinetics |
No specific toxicity data have been reported for FATP1-IN-1. As a research compound, it should be handled with standard laboratory safety precautions. Its safety profile has not been evaluated for human use.
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| References |
[1]. Matsufuji T, et al. Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties. Bioorg Med Chem Lett. 2013;23(9):2560-2565.
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| Additional Infomation |
FATP1-IN-1 is a research compound, not an approved drug. It is a potent and selective inhibitor of fatty acid transport protein 1 (FATP1), used as a chemical tool to study the role of FATP1 in lipid metabolism and metabolic diseases.
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| Molecular Formula |
C18H22FN5OS
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|---|---|
| Molecular Weight |
375.46
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| Exact Mass |
375.152
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| CAS # |
1431945-95-7
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| PubChem CID |
71601847
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC2=C(C1)N=C(S2)NC(=O)CN3CCN(CC3)C4=NC=C(C=C4)F
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| InChi Key |
ORQHHLPTMSGMQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22FN5OS/c19-13-5-6-16(20-11-13)24-9-7-23(8-10-24)12-17(25)22-18-21-14-3-1-2-4-15(14)26-18/h5-6,11H,1-4,7-10,12H2,(H,21,22,25)
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| Chemical Name |
2-[4-(5-fluoropyridin-2-yl)piperazin-1-yl]-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)acetamide
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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: 62.5 mg/mL (166.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.54 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (20.8 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (5.54 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (20.8 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6634 mL | 13.3170 mL | 26.6340 mL | |
| 5 mM | 0.5327 mL | 2.6634 mL | 5.3268 mL | |
| 10 mM | 0.2663 mL | 1.3317 mL | 2.6634 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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