| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| Other Sizes |
| Targets |
HSL[1].
Hormone-sensitive lipase (HSL). Its selectivity for HSL makes it a valuable probe for studying lipolysis and lipid metabolism. |
|---|---|
| ln Vitro |
HSL-IN-3 is a selective inhibitor of HSL with an IC50 of 100 nM. Its activity is measured by its ability to inhibit the enzymatic hydrolysis of triglycerides by HSL. It is a boronic acid derivative, suggesting a mechanism involving covalent or reversible interaction with the active site serine residue of the lipase.
|
| ln Vivo |
In vivo, HSL-IN-3 has anti-obesity and metabolic regulatory effects. By inhibiting HSL, it reduces the breakdown of stored triglycerides into free fatty acids, thereby affecting energy homeostasis and lipid availability. This can be studied in animal models of obesity and insulin resistance.
|
| Enzyme Assay |
The activity of HSL-IN-3 is typically assessed using a purified HSL enzyme assay. The enzyme is incubated with a fluorogenic or radiolabeled substrate in the presence of varying concentrations of the inhibitor. The residual enzyme activity is measured, and the IC50 value (100 nM) is determined from a dose-response curve.
|
| Cell Assay |
Cellular studies involve treating adipocytes or other cell lines with HSL-IN-3 and measuring the release of free fatty acids and glycerol into the culture medium, which are products of lipolysis. The compound's effect on lipid droplet morphology can also be assessed using microscopy and lipid-specific stains.
|
| Animal Protocol |
In vivo studies typically involve administering HSL-IN-3 to animal models of metabolic disease, such as diet-induced obese mice. Parameters like body weight, food intake, serum free fatty acid and triglyceride levels, and insulin sensitivity are monitored to assess the compound's efficacy.
|
| ADME/Pharmacokinetics |
Specific ADME data for HSL-IN-3 are not extensively published. It is soluble in DMSO (≥200 mg/mL) and as a powder, it is stable at -20°C for 3 years. Its properties as a small molecule (MW 262.11) suggest it would be absorbed and metabolized, but detailed pharmacokinetic studies would be needed.
|
| Toxicity/Toxicokinetics |
Toxicological data for HSL-IN-3 are not widely available in general reference materials. As a research compound, it is not intended for human use. Standard laboratory safety precautions apply. Its safety profile would be established through dedicated toxicology studies if it were to be developed further.
|
| References | |
| Additional Infomation |
HSL-IN-3 is a research compound used as a pharmacological tool to study the role of HSL in lipid metabolism and related diseases. It is not approved for clinical use. Its development highlights the interest in HSL as a therapeutic target for obesity, insulin resistance, and other metabolic disorders.
|
| Molecular Formula |
C14H19BO4
|
|---|---|
| Molecular Weight |
262.11
|
| Exact Mass |
262.137
|
| CAS # |
346656-34-6
|
| PubChem CID |
10332902
|
| Appearance |
Colorless to light yellow liquid
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
384.8±25.0 °C at 760 mmHg
|
| Flash Point |
186.5±23.2 °C
|
| Vapour Pressure |
0.0±0.9 mmHg at 25°C
|
| Index of Refraction |
1.499
|
| LogP |
1.631
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
19
|
| Complexity |
309
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1B(C2=C([H])C([H])=C([H])C([H])=C2C(=O)OC([H])([H])C([H])([H])[H])OC([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C1([H])[H]
|
| InChi Key |
GZHASWCTAWNFFW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H19BO4/c1-4-17-13(16)11-7-5-6-8-12(11)15-18-9-14(2,3)10-19-15/h5-8H,4,9-10H2,1-3H3
|
| Chemical Name |
ethyl 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)benzoate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (381.52 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.94 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 (7.94 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 (7.94 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 | 3.8152 mL | 19.0760 mL | 38.1519 mL | |
| 5 mM | 0.7630 mL | 3.8152 mL | 7.6304 mL | |
| 10 mM | 0.3815 mL | 1.9076 mL | 3.8152 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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