Nicodicosapent

Name: Nicodicosapent
Brand: MedChemExpress
SKU: HY-17640
Rating: 4.5 (1 reviews)

Cat. No.: HY-17640 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Nicodicosapent Chemical Structure

CAS No. : 1269181-69-2

Size	Price	Stock	Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 214	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 214	In-stock	Estimated Time of Arrival: December 31
Solid or liquid
2 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 216	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1080	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	17 μM Compound: 5	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	[PMID: 26784936]
HepG2	IC₅₀	27 μM Compound: 5	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	[PMID: 26784936]

In Vitro

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.

In Vivo

Nicodicosapent (100 mg/kg po) produces high plasma levels of nicotinuric acid in the plasma. ApoE*3-Leiden mice treated with Nicodicosapent show a significant reduction in PCSK9 levels, LDL particles including VLDL and LDL cholesterol, as well as plasma triglycerides^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

449.63

Formula

C₂₈H₃₉N₃O₂

CAS No.

1269181-69-2

Appearance

Solid-Liquid Mixture

Color

Yellow to brown

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (222.41 mM; 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)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2241 mL	11.1203 mL	22.2405 mL
5 mM	0.4448 mL	2.2241 mL	4.4481 mL
10 mM	0.2224 mL	1.1120 mL	2.2241 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.75 mg/mL (8.34 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (268 KB) SDS (252 KB)

COA (237 KB) HNMR (489 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Vu CB, et al. Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid. J Med Chem. 2016 Feb 11;59(3):1217-31. [Content Brief]

Animal Administration
^[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Vu CB, et al. Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid. J Med Chem. 2016 Feb 11;59(3):1217-31. [Content Brief]

Complete Stock Solution Preparation Table

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
Ethanol / DMSO	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

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nicodicosapent1269181-69-2Fatty Acid Synthase (FASN)AutophagyInhibitorinhibitorinhibit

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Nicodicosapent

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