ELOVL6-IN-5
Based on 1 Customer Validation
ELOVL6-IN-5 is an orally active and selective elongase enzyme of long-chain fatty acid family 6 (ELOVL6) inhibitor with IC50 values of 85 nM and 38 nM for human and mouse ELOVL6, respectively. ELOVL6-IN-5 shows >60-fold selectivity over other ELOVL family enzymes (ELOVL1, 2, 3, 5) and no effect on other lipid synthesis enzymes like ACC1, ACC2. ELOVL6-IN-5 reduces hepatic fatty acid composition ratio of C18 to C16 in diet-induced obesity (DIO) and KKAy mice. ELOVL6 inhibition by ELOVL6-IN-5 does not improve insulin resistance. ELOVL6-IN-5 can be used for the research of metabolic disease.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 95.47%
- CAS. Nr.: 1135000-36-0
- Formel: C20H20F3N3O3S
- Molecular Weight:439.45
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
ELOVL-6 85 nM (IC50, Human) |
ELOVL-6 38 nM (IC50, Mouse) |
In Vitro
ELOVL6-IN-5 (compound B) (1 h pre-incubation; 4 h with [14C] palmitic acid) reduces fatty acid elongation index in mouse hepatoma H2.35 cells (IC50 = 30.4 nM)[1].
ELOVL6-IN-5 shows the mode-of-action of an ELOVL6 inhibitor in a non-competitive manner for malonyl-CoA and in an un-competitive manner for palmitoyl-CoA. ELOVL6-IN-5 has no effect on recombinantly expressed human lipid synthesis enzymes, ACC1 and ACC2. ELOVL6-IN-5 does not affect fatty acid synthesis in rat primary hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
ELOVL6-IN-5 (100 mg/kg, 0.13% in diet; p.o.; twice daily; 28 days) reduces hepatic C18/C16 fatty acid ratio but shows no beneficial metabolic effects in KKAy mice with 24-h inhibition regimen[1].
ELOVL6-IN-5 (30 mg/kg; p.o.; twice daily; 14 days) reduces hepatic C18/C16 fatty acid ratio but shows no beneficial metabolic effects in C57BL/6J diet-induced obesity mice[1].
ELOVL6-IN-5 (30 mg/kg; p.o.; twice daily; 28 days) reduces hepatic C18/C16 fatty acid ratio but shows no beneficial metabolic effects in KKAy mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (Male) were interperitoneally administered Palmitic acid (HY-N0830).[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:p.o.; single dose
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Result:Reduced the hepatic fatty acid elongation index to 73% (1 mg/kg), 39% (3 mg/kg), 30% (10 mg/kg) of control.
3 mg/kg and 10 mg/kg doses showed significant reduction compared to vehicle control.
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Animal Model:KKAy (Male, induced by regular diet)[1]
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Dosage:100 mg/kg, 0.13% (w/w) in diet
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Administration:p.o.; twice daily; 28 days
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Result:Significantly reduced the ratio of hepatic C18/C16 fatty acid.
Showed no effect on body fat, plasma insulin, liver triglyceride content, or oral glucose tolerance test AUC glucose compared to vehicle control.
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Animal Model:C57BL/6J (Male, induced by high-fat diet for 7 months)[1]
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Dosage:30 mg/kg
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Administration:p.o.; twice daily; 14 days
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Result:Significantly reduced the ratio of hepatic C18/C16 fatty acid.
Showed no effect on body fat, plasma insulin, plasma leptin, liver triglyceride content, or intraperitoneal glucose tolerance test AUC glucose compared to vehicle control.
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Animal Model:KKAy (Male, induced by regular diet)[1]
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Dosage:30 mg/kg
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Administration:p.o.; twice daily; 28 days
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Result:Significantly reduced the ratio of hepatic C18/C16 fatty acid.
Showed no effect on body fat, plasma insulin, plasma leptin, liver triglyceride content, or intraperitoneal glucose tolerance test AUC glucose compared to vehicle control.
Chemical Information
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CAS. Nr. 1135000-36-0
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Appearance Solid
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Molecular Weight 439.45
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Formel C20H20F3N3O3S
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Color White to off-white
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SMILES
O=C(N1C2CCC1CC(S(=O)(C3=NC=CC=C3)=O)C2)NC4=CC=C(C(F)(F)F)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 100 mg/mL (227.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2756 mL | 11.3779 mL | 22.7557 mL | 56.8893 mL |
| 5 mM | 0.4551 mL | 2.2756 mL | 4.5511 mL | 11.3779 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2756 mL | 5.6889 mL | |
| 15 mM | 0.1517 mL | 0.7585 mL | 1.5170 mL | 3.7926 mL | |
| 20 mM | 0.1138 mL | 0.5689 mL | 1.1378 mL | 2.8445 mL | |
| 25 mM | 0.0910 mL | 0.4551 mL | 0.9102 mL | 2.2756 mL | |
| 30 mM | 0.0759 mL | 0.3793 mL | 0.7585 mL | 1.8963 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5689 mL | 1.4222 mL | |
| 50 mM | 0.0455 mL | 0.2276 mL | 0.4551 mL | 1.1378 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3793 mL | 0.9482 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7111 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2276 mL | 0.5689 mL |
ELOVL6-IN-5 Related Classifications
HY-160912 Related Classifications
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