| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
HSL-IN-5 targets hormone-sensitive lipase (HSL), an enzyme that hydrolyzes triglycerides to release free fatty acids for energy production. It plays a key role in lipid metabolism and is a therapeutic target for obesity and type 2 diabetes. As an inhibitor with an IC50 of 0.25 microM, HSL-IN-5 blocks the breakdown of triglycerides in adipose tissue, thereby reducing the release of free fatty acids into the bloodstream.
|
|---|---|
| ln Vitro |
HSL-IN-5 is a potent inhibitor of hormone-sensitive lipase (HSL) with an IC50 of 0.25 microM (250 nM). This indicates that it effectively inhibits the enzyme at low micromolar concentrations. By blocking HSL activity, the compound prevents the lipolysis of triglycerides and the subsequent release of free fatty acids. This mechanism is being investigated for the treatment of diabetes and metabolic syndrome, as elevated free fatty acids contribute to insulin resistance.
|
| ln Vivo |
HSL-IN-5 is used in research for diabetes, suggesting that it has shown efficacy in animal models of the disease. While specific in vivo data is not provided, inhibitors of hormone-sensitive lipase are generally expected to improve insulin sensitivity and lower blood glucose levels in diabetic animal models. The compound's IC50 of 0.25 microM suggests it could be effective at relatively low doses.
|
| Enzyme Assay |
The inhibitory activity of HSL-IN-5 is measured using a cell-free HSL enzyme assay. Procedure: Recombinant human hormone-sensitive lipase (HSL, 10 ng) is incubated with varying concentrations of HSL-IN-5 (0.001-10 microM) in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 5 mM MgCl2, 1 mM DTT, 0.1% BSA). The reaction is initiated by adding a fluorogenic substrate, such as 4-methylumbelliferyl oleate (4-MU oleate, 20 microM). After 30-60 minutes at 37degC, the fluorescence of the released 4-methylumbelliferone (4-MU) is measured (excitation 360 nm, emission 460 nm). The IC50 is calculated as the concentration that inhibits 50% of the fluorescence increase compared to the control. The reported IC50 is 0.25 microM.
|
| Cell Assay |
The cellular activity of HSL-IN-5 can be assessed in 3T3-L1 adipocytes. Procedure: 3T3-L1 preadipocytes are differentiated into mature adipocytes over 8-10 days. Differentiated adipocytes are seeded in 96-well plates and serum-starved for 2 hours. Cells are pre-treated with varying concentrations of HSL-IN-5 (0.1-10 microM) for 30 minutes, then stimulated with isoproterenol (1 microM) to induce lipolysis. After 2-4 hours, the culture medium is collected, and glycerol release (a measure of lipolysis) is measured using a colorimetric Free Glycerol Reagent. The IC50 for inhibition of lipolysis is calculated. Additionally, intracellular triglyceride levels can be measured by Oil Red O staining. A reduction in glycerol release indicates cellular efficacy.
|
| Animal Protocol |
The in vivo efficacy of HSL-IN-5 can be evaluated in a mouse model of diet-induced obesity (DIO). Procedure: Male C57BL/6J mice are fed a high-fat diet (60% kcal from fat) for 12-16 weeks to induce obesity and insulin resistance. Mice are randomized into groups (n=10). HSL-IN-5 is formulated in a suitable vehicle (e.g., 0.5% methylcellulose) and administered orally at doses of 10, 30, and 100 mg/kg once daily for 4 weeks. Body weight, food intake, and fasting blood glucose are measured weekly. An oral glucose tolerance test (OGTT) is performed at week 2. At study endpoint, blood is collected for serum free fatty acids (FFA), triglyceride, and insulin measurements. A reduction in body weight, fasting glucose, and serum FFA indicates efficacy.
|
| ADME/Pharmacokinetics |
Specific PK data for HSL-IN-5 is not provided. As a small molecule with a molecular weight of 388.38 g/mol, it is expected to have moderate oral bioavailability. The compound is soluble in DMSO at 100 mg/mL. For in vivo studies, it is likely formulated in vehicles such as 0.5% methylcellulose for oral administration. The compound is stored as a powder at -20degC.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for HSL-IN-5 is not provided. As a research chemical, it is not intended for human use. Potential adverse effects of HSL inhibition may include steatosis (fatty liver) due to reduced lipolysis and altered lipid metabolism. Standard safety precautions for handling research chemicals should be followed. The compound is for research use only.
|
| References | |
| Additional Infomation |
HSL-IN-5 (Example 21, WAY659100) is a hormone-sensitive lipase (HSL) inhibitor with an IC50 of 0.25 microM. It is used in research for diabetes and metabolic disorders. The compound is stored as a powder at -20degC. It is for research use only and is not an approved drug.
|
| Molecular Formula |
C18H23F3N2O4
|
|---|---|
| Molecular Weight |
388.38
|
| CAS # |
308830-70-8
|
| Appearance |
White to off-white solid powder
|
| SMILES |
N1(C(OC(C)(C)C)=O)CCC(C(NC2=CC=C(OC(F)(F)F)C=C2)=O)CC1
|
| 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 (~257.48 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5748 mL | 12.8740 mL | 25.7480 mL | |
| 5 mM | 0.5150 mL | 2.5748 mL | 5.1496 mL | |
| 10 mM | 0.2575 mL | 1.2874 mL | 2.5748 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
