| 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 |
ELOVL6 is a key enzyme in the elongation of long-chain fatty acids, converting palmitate (C16:0) to stearate (C18:0). Inhibition of ELOVL6 is a therapeutic strategy for metabolic diseases such as obesity, diabetes, and non-alcoholic fatty liver disease (NAFLD).
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| ln Vitro |
ELOVL6-IN-4 (compound 1w) efficiently lowers the mouse hepatocytes' elongation index (H2.35) at an IC50 of 30 nM.
In vitro, ELOVL6-IN-4 potently inhibits human and mouse ELOVL6 with IC50s of 79 nM and 94 nM, respectively. It exhibits excellent selectivity over other human ELOVL isoforms (ELOVL1, -2, -3, -5) and mouse ELOVL3. |
| ln Vivo |
ELOVL6-IN-4 (compound 1w; 1-10 mg/kg; gavage, single dose) can reduce the mouse liver's elongation index in an efficient and dose-dependent manner [1].
A non-cell assay uses microsomes expressing human or mouse ELOVL6. The enzyme is incubated with [14C]-malonyl-CoA and palmitoyl-CoA (C16:0). ELOVL6-IN-4 is added, and the formation of stearoyl-CoA (C18:0) is quantified by TLC or LC-MS. |
| Cell Assay |
For cell studies, ELOVL6-IN-4 is dissolved in DMSO and diluted in culture medium. Cells (e.g., hepatocytes, adipocytes) are treated with the compound for 24-48 hours. Fatty acid composition is analyzed by GC-MS to assess inhibition of C18:0 synthesis.
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice[1]
Doses: 1 mg/kg, 3 mg/kg, and 10 mg/kg Route of Administration: Oral administration; once Experimental Results: Potently and dose-dependently suppressed the elongation index in the liver in mice . In animal studies, ELOVL6-IN-4 (1-10 mg/kg; gavage, single dose) can reduce the mouse liver's elongation index (C18:0/C16:0 ratio) in an efficient and dose-dependent manner. It is used in models of diet-induced obesity and NAFLD. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies in rodents show good oral bioavailability and a favorable half-life. The compound is suitable for in vivo efficacy studies.
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| Toxicity/Toxicokinetics |
In preclinical studies, ELOVL6-IN-4 is well-tolerated at efficacious doses. No significant toxicity has been reported.
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| References |
[1]. Tsuyoshi Nagase, et al. Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors. J Med Chem. 2009 Jul 23;52(14):4111-4.
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| Additional Infomation |
ELOVL6-IN-4 is a research tool for studying the role of ELOVL6 in lipid metabolism. It has potential therapeutic applications in metabolic diseases such as obesity, insulin resistance, and fatty liver disease. It is not an approved drug.
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| Molecular Formula |
C20H20F3N3O3S
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|---|---|
| Molecular Weight |
439.45
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| Exact Mass |
439.118
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| CAS # |
1170321-92-2
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| PubChem CID |
25234001
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| Appearance |
White to off-white solid powder
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| LogP |
5.193
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
718
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC2CC(CC1N2C(=O)NC3=CC=C(C=C3)C(F)(F)F)S(=O)(=O)C4=CC=CC=N4
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| InChi Key |
WYCGDOXAJCYGEC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20F3N3O3S/c21-20(22,23)13-4-6-14(7-5-13)25-19(27)26-15-8-9-16(26)12-17(11-15)30(28,29)18-3-1-2-10-24-18/h1-7,10,15-17H,8-9,11-12H2,(H,25,27)
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| Chemical Name |
3-pyridin-2-ylsulfonyl-N-[4-(trifluoromethyl)phenyl]-8-azabicyclo[3.2.1]octane-8-carboxamide
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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: ~50 mg/mL (~113.8 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.69 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 2.5 mg/mL (5.69 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 2.5 mg/mL (5.69 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2756 mL | 11.3779 mL | 22.7557 mL | |
| 5 mM | 0.4551 mL | 2.2756 mL | 4.5511 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2756 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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