| 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 |
Insulin-regulated aminopeptidase (IRAP); also inhibits other aminopeptidase activities.
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|---|---|
| ln Vitro |
HFI-142 inhibits IRAP with a Ki of 2.01 µM. It also inhibits leukotriene A4 biosynthesis in erythrocytes. The compound shows activity against other aminopeptidases. These activities suggest potential roles in modulating inflammatory and metabolic pathways. Specific IC50 values for related aminopeptidases are not detailed in public search results.
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| ln Vivo |
In vivo efficacy of HFI-142 has not been extensively characterized. Based on its in vitro activities, the compound may have potential in models of cancer and inflammation through modulation of aminopeptidase activity and leukotriene biosynthesis. Specific animal model data are limited in publicly available literature.
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| Enzyme Assay |
IRAP inhibition is assessed using in vitro enzyme assays with recombinant IRAP and a fluorogenic substrate. Ki values are calculated from enzyme kinetics. Aminopeptidase activity is measured by following the release of fluorescent products. Leukotriene A4 biosynthesis is measured in erythrocyte lysates using HPLC or mass spectrometry.
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| Cell Assay |
Cellular activity is evaluated in erythrocytes or cancer cell lines. Cells are treated with HFI-142 at various concentrations and leukotriene A4 biosynthesis is measured. Aminopeptidase activity is assessed in cell lysates using fluorogenic substrates. Effects on inflammatory and metabolic pathways are measured by qRT-PCR or Western blot for relevant markers.
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| Animal Protocol |
In vivo studies for HFI-142 are limited. Potential studies could be conducted in mouse models of cancer or inflammation. The compound would be administered orally or via intraperitoneal injection. Tumor growth, inflammatory markers, and metabolic parameters would be assessed. Specific protocols are not detailed in publicly available literature.
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| ADME/Pharmacokinetics |
HFI-142 has a molecular formula of C17H16N2O4 and molecular weight of 312.32. It is soluble in DMSO (31.23 mg/mL). Storage: powder at -20°C for up to 3 years or at 4°C for 2 years. The compound is a small molecule aminopeptidase inhibitor.
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| Toxicity/Toxicokinetics |
Safety data for HFI-142 indicate it is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity, organ toxicity, and genotoxicity are not extensively published. Standard laboratory safety practices should be followed during handling.
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| References | |
| Additional Infomation |
HFI-142 is a research tool compound for studying IRAP and aminopeptidase biology. It is not approved for clinical use. The compound has been investigated for potential applications in cancer research due to its effects on leukotriene biosynthesis and inflammatory pathways.
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| Molecular Formula |
C17H16N2O4
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|---|---|
| Molecular Weight |
312.319944381714
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| Exact Mass |
312.111
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| CAS # |
332164-34-8
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| PubChem CID |
655457
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(C1=C(N)OC2=CC(=CC=C2C1C1=CC=CN=C1)O)=O
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| InChi Key |
JOPNHSIHFSZJMB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16N2O4/c1-2-22-17(21)15-14(10-4-3-7-19-9-10)12-6-5-11(20)8-13(12)23-16(15)18/h3-9,14,20H,2,18H2,1H3
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| Chemical Name |
ethyl 2-amino-7-hydroxy-4-pyridin-3-yl-4H-chromene-3-carboxylate
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| Synonyms |
HFI142; HFI 142; HFI-142
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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 : ~125 mg/mL (~400.23 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.66 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 (6.66 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 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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