| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Hormone-sensitive lipase (HSL) is the primary target of Hi 76-0079. HSL is an intracellular lipase that plays a key role in the breakdown of stored triglycerides in adipose tissue. It is also involved in the hydrolysis of cholesteryl esters in steroidogenic tissues. Hi 76-0079 is a specific HSL inhibitor, showing no significant effect on other lipases such as ATGL at concentrations up to 50 µM.
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| ln Vitro |
Hi 76-0079 is a potent HSL inhibitor with an IC₅₀ value of 184 nM (0.184 µM). Another source reports an IC₅₀ of 0.1 µM (100 nM). It has been shown to synergize with the ATGL inhibitor Atglistatin to block lipolysis in vitro. Hi 76-0079 is a selective compound, as it does not affect ATGL or other lipases at high concentrations (IC₅₀ >50 µM).
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| ln Vivo |
In vivo, Hi 76-0079 is a potential compound for studying and preventing obesity and diabetes. As an HSL inhibitor, it is expected to reduce the release of free fatty acids from adipose tissue, thereby improving insulin sensitivity and reducing lipid accumulation. It has been identified as a research tool for in vivo metabolic studies.
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| Enzyme Assay |
The activity of Hi 76-0079 is assessed via enzyme inhibition assays. A common method involves pre-incubating the enzyme (HSL) with the inhibitor (up to 50 µM) for 30-70 minutes at room temperature. Following this, an emulsified fluorescently labeled triglyceride analog substrate is added, and the reduction in enzymatic hydrolysis is measured. The compound's IC₅₀ is determined from these assays.
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| Cell Assay |
Cell-based assays for Hi 76-0079 have been performed using lysates of HEK293A cells that overexpress Lipe (the gene for HSL). In these lysates, the compound's ability to inhibit the hydrolysis of the substrate p-nitrophenyl butyrate (PNPB) was measured, yielding an IC₅₀ of 0.1 μM. It has also been used in synergy studies with the ATGL inhibitor Atglistatin.
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| Animal Protocol |
In vivo studies of Hi 76-0079 are focused on metabolic research, particularly in models of obesity and diabetes. The compound is administered to animals to investigate the effects of HSL inhibition on lipid metabolism, insulin sensitivity, and overall energy homeostasis. As a substrate inhibitor, its effects are expected to be reversible as the enzyme hydrolyzes the inhibitor.
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| ADME/Pharmacokinetics |
Hi 76-0079 has a molecular weight of 256.69 g/mol and the formula C₁₁H₁₃ClN₂O₃. It is soluble in DMSO. The CAS number is 374567-94-9. It is a white to off-white solid. For storage, it is stable as a powder at -20°C for up to 3 years, and in solution at -80°C for 6 months.
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| Toxicity/Toxicokinetics |
Toxicological data for Hi 76-0079 are not extensively documented. As a research chemical, it is handled with standard laboratory safety precautions. Its potential for use in obesity and diabetes research suggests it has been evaluated for safety in preclinical models, though specific toxicity profiles are not publicly available.
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| References | |
| Additional Infomation |
Hi 76-0079 (NNC0076-0079) is a potent and selective inhibitor of hormone-sensitive lipase (HSL). It is a research compound developed to study lipid metabolism, with potential applications in obesity and diabetes research. Its unique mechanism as a substrate inhibitor makes it a valuable tool for investigating the role of HSL in various physiological and pathological processes.
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| Molecular Formula |
C11H13N2O3CL
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|---|---|
| Molecular Weight |
256.686
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| Exact Mass |
256.061
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| CAS # |
374567-94-9
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| PubChem CID |
9856441
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| Appearance |
White to off-white solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
251
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCN(NC(=O)OC2=CC=C(Cl)C=C2)CC1
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| InChi Key |
CJKVBAQMCNYASH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H13ClN2O3/c12-9-1-3-10(4-2-9)17-11(15)13-14-5-7-16-8-6-14/h1-4H,5-8H2,(H,13,15)
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| Chemical Name |
(4-chlorophenyl) N-morpholin-4-ylcarbamate
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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: 250 mg/mL (973.94 mM)
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| 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 | 3.8957 mL | 19.4787 mL | 38.9575 mL | |
| 5 mM | 0.7791 mL | 3.8957 mL | 7.7915 mL | |
| 10 mM | 0.3896 mL | 1.9479 mL | 3.8957 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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