| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
The primary target of HSL-IN-1 is hormone-sensitive lipase (HSL), a key enzyme in lipid mobilization and triglyceride hydrolysis. HSL catalyzes the breakdown of stored triglycerides into free fatty acids and glycerol, playing a central role in energy homeostasis. HSL-IN-1 acts as a potent and orally active inhibitor of HSL with an IC₅0 of 2 nM. By inhibiting HSL, the compound reduces the release of free fatty acids from adipose tissue. HSL is a validated target for metabolic disorders such as obesity, diabetes, and cardiovascular diseases.
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| ln Vitro |
In vitro studies demonstrate that HSL-IN-1 is a potent inhibitor of HSL with an IC₅0 of 2 nM. The compound significantly reduces the reactive metabolite load and can reduce the release of free fatty acids from stored fat. HSL-IN-1 is an orally active compound, making it suitable for in vivo studies. Its potent inhibitory activity makes it a valuable tool for studying lipid metabolism, energy regulation, and metabolic disorders. The compound is widely used in research on obesity, diabetes, and cardiovascular diseases.
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| ln Vivo |
In vivo studies of HSL-IN-1 are focused on evaluating its efficacy in animal models of metabolic disorders. As an orally active and potent HSL inhibitor with an IC₅0 of 2 nM, the compound is expected to demonstrate significant effects on lipid metabolism and energy homeostasis in vivo. HSL-IN-1 may be used to study the role of HSL in obesity, diabetes, and cardiovascular diseases. By reducing free fatty acid release from adipose tissue, the compound could improve insulin sensitivity and metabolic parameters. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, HSL-IN-1 is evaluated using lipase activity assays that measure the hydrolysis of triglycerides or other substrates by HSL. The compound is incubated with recombinant HSL enzyme and a suitable substrate at various concentrations. HSL activity is quantified by measuring the release of free fatty acids or glycerol using colorimetric, fluorometric, or radiometric methods. IC₅0 values are determined from dose-response curves. Selectivity profiling against other lipases may be performed to confirm specificity. Standard assay conditions include physiological buffer systems with appropriate pH and ionic strength.
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| Cell Assay |
For in vitro cellular experiments, HSL-IN-1 is tested in adipocytes or other cell lines to evaluate its effects on lipolysis and lipid metabolism. Cells are cultured in appropriate media and treated with various concentrations of the compound (typically ranging from nanomolar to micromolar). Lipolysis is assessed by measuring the release of free fatty acids and glycerol into the culture medium. The compound's effects on cellular lipid content and energy metabolism are further investigated. Cell viability is monitored. The compound's effects on HSL activity in cells can be confirmed by measuring HSL phosphorylation or activity.
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| Animal Protocol |
For in vivo animal experiments, HSL-IN-1 can be administered to rodents via oral gavage, taking advantage of its oral bioavailability. The compound can be evaluated in models of obesity, diabetes, and metabolic syndrome. Typical dosing regimens may range from 0.1 to 10 mg/kg depending on the study objectives. Parameters such as body weight, food intake, glucose tolerance, insulin sensitivity, and lipid profiles are measured. Tissue samples are collected for analysis of lipid content, HSL activity, and metabolic markers. Pharmacodynamic markers such as free fatty acid levels are measured in plasma.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HSL-IN-1 include oral activity, supporting its administration via oral gavage in vivo. As a small molecule with a molecular weight of 436.58 g/mol, it is likely to have reasonable absorption and distribution characteristics. The compound significantly reduces the reactive metabolite load, suggesting favorable metabolic stability. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies. The compound's protein binding and excretion pathways remain to be fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for HSL-IN-1 are limited, as it is primarily a research tool. As an HSL inhibitor, its toxicity would depend on the importance of HSL for normal lipid metabolism and energy homeostasis. HSL plays a central role in the mobilization of stored fats, and its inhibition could affect energy balance and metabolic regulation. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound, including the use of personal protective equipment and adherence to institutional safety guidelines.
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| References | |
| Additional Infomation |
HSL-IN-1 is a research compound used to study lipid metabolism and metabolic disorders. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a potent and orally active HSL inhibitor with an IC₅0 of 2 nM that significantly reduces reactive metabolite load and free fatty acid release. It is widely used in research on obesity, diabetes, and cardiovascular diseases.
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| Molecular Formula |
C19H13BCLF3N2O4
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|---|---|
| Molecular Weight |
436.576734304428
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| Exact Mass |
436.06
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| CAS # |
2095156-13-9
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| PubChem CID |
132569642
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
579
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=C(B(O)O)C=1)NC(C1=CN=C(C=C1)OC1C=CC(C(F)(F)F)=CC=1)=O
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| InChi Key |
PDMXSCCBEBCTGX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H13BClF3N2O4/c21-13-4-7-16(15(9-13)20(28)29)26-18(27)11-1-8-17(25-10-11)30-14-5-2-12(3-6-14)19(22,23)24/h1-10,28-29H,(H,26,27)
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| Chemical Name |
[5-chloro-2-[[6-[4-(trifluoromethyl)phenoxy]pyridine-3-carbonyl]amino]phenyl]boronic acid
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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 : ~12.5 mg/mL (~28.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.86 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 12.5 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: ≥ 1.25 mg/mL (2.86 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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2905 mL | 11.4527 mL | 22.9053 mL | |
| 5 mM | 0.4581 mL | 2.2905 mL | 4.5811 mL | |
| 10 mM | 0.2291 mL | 1.1453 mL | 2.2905 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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