Nicodicosapent
Based on 1 Customer Validation
Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.
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- Pureté: 99.79%
- CAS No.: 1269181-69-2
- Formule: C28H39N3O2
- Masse moléculaire:449.63
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Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
17 μM
Compound: 5
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Inhibition of SREBP2 in human HepG2 cells assessed as reduction of PCSK9 secretion after 16 hrs by ELISA
Inhibition of SREBP2 in human HepG2 cells assessed as reduction of PCSK9 secretion after 16 hrs by ELISA
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[PMID: 26784936] |
| HepG2 | IC50 |
27 μM
Compound: 5
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Inhibition of ApoB secretion in human HepG2 cells after 16 hrs by ELISA
Inhibition of ApoB secretion in human HepG2 cells after 16 hrs by ELISA
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[PMID: 26784936] |
Nicodicosapent decreases the production of mature SREBP-2 protein in HepG2 cells, but does not interact with the GPR109A receptor. Nicodicosapent shows a synergistic inhibition on secreted PCSK9 and has an IC50 value of 17 μM. Nicodicosapent significantly inhibits ApoB secretion in a dose-dependent manner with IC50 of 27 μM. Nicodicosapent results in a time-dependent hydrolysis in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1269181-69-2
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Appearance Solid-Liquid Mixture
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Masse moléculaire 449.63
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Formule C28H39N3O2
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Color Yellow to brown
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SMILES
O=C(C1=CC=CN=C1)NCCNC(CCC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CC)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvant et solubilité
DMSO : 100 mg/mL (222.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 3.33 mg/mL (7.41 mM; Need ultrasonic)
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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 3 mg/mL (6.67 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 3 mg/mL (6.67 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Protocole
Male Sprague-Dawley rats (n=4/treatment group) are administered with a single oral dose of either niacin (30 mg/kg) or Nicodicosapent (100 mg/kg). Compounds are formulated as an aqueous emulsion using Tween, Peceol, PEG400, and tocopherol. Nicodicosapent (170 mg) is formulated in 2.38 g of the oil mixture containing 40% Tween, 50% Peceol, 10% PEG400, and 0.2% tocopherol. The concentration of 5 in oil is 66 mg/g of oil. For oral dosing, this oil formulation is then diluted with 14.25 mL of water to form a 10 mg/mL drug emulsion and dosed as an oral gavage. Collection time points are 5, 15, and 30 min 1, 2, 4, 6, and 8 h postdose. Blood samples are collected via saphenous vein and placed in tubes containing paraoxon (10 μL of a 200 μM solution in DMSO) and stored on an ice block until centrifuged at 8000 rpm for 6 min at 2-8°C. The resulting plasma is kept frozen at −80°C until analysis. Nicodicosapent, nicotinic acid, and nicotinuric acid standard curves are generated to allow for quantitative analysis of plasma samples. Standard curves are generated by adding 10 μL of a given compound in methanol (50 μg/mL) to 50 μL of blank plasma in a 96-well microplate, resulting in the following final concentration range: 8333, 2083, 521, 130.2, 32.5, 8.1, 2.0, and 0.5 ng/mL. Then 300 μL of acetonitrile containing 100 ng/mL of an internal standard is added to each sample. The 96-well microplate is vortexed for 30 s and is then centrifuged for 45 min at 2300 g. Then 100 μL of supernatant is transferred from each sample to an empty 96-well microplate for analysis by LC/MS/MS. The instrument used is an Agilent liquid chromatograph equipped with a binary pump (1200 series), an autosampler (1200 series), and a degasser (1200 series). Mass spectrometric analysis is performed using an Agilent 6410 triple quadrupole with an ESI interface. The data acquisition and quantitation is done with Agilent Masshunter software. The column used is a Phenomenex Gemini C6 Phenyl 110A 50 mm×4.6 mm, 1.8 μm. The following mobile phase gradient is used (water = solvent A; methanol = solvent B): 0.01 min=45%A/55%B; 0.5 min=45%A/55%B; 1 min=5%A/95%B; 3.5 min=5%A/95%B; 3.51 min=45%A/55%B; 4 min=45%A/55%B.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (268 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (stored under nitrogen). 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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.2241 mL | 11.1203 mL | 22.2405 mL | 55.6013 mL |
| 5 mM | 0.4448 mL | 2.2241 mL | 4.4481 mL | 11.1203 mL | |
| DMSO | 10 mM | 0.2224 mL | 1.1120 mL | 2.2241 mL | 5.5601 mL |
| 15 mM | 0.1483 mL | 0.7414 mL | 1.4827 mL | 3.7068 mL | |
| 20 mM | 0.1112 mL | 0.5560 mL | 1.1120 mL | 2.7801 mL | |
| 25 mM | 0.0890 mL | 0.4448 mL | 0.8896 mL | 2.2241 mL | |
| 30 mM | 0.0741 mL | 0.3707 mL | 0.7414 mL | 1.8534 mL | |
| 40 mM | 0.0556 mL | 0.2780 mL | 0.5560 mL | 1.3900 mL | |
| 50 mM | 0.0445 mL | 0.2224 mL | 0.4448 mL | 1.1120 mL | |
| 60 mM | 0.0371 mL | 0.1853 mL | 0.3707 mL | 0.9267 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2780 mL | 0.6950 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2224 mL | 0.5560 mL |
Nicodicosapent Related Classifications
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