CP-24879 (hydrochloride)

Name: CP-24879 hydrochloride
Brand: MedChemExpress
SKU: HY-115319
Rating: 5.0 (2 reviews)

製品番号: HY-115319 純度: 99.59%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

CP-24879 (hydrochloride) is a potent, selective and combined delta5D/delta6D inhibitor. CP-24879 (hydrochloride) can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 (hydrochloride) exhibits superior antisteatotic and anti-inflammatory actions in fat-1 and ω-3-treated hepatocytes, and can be used for non-alcoholic steatohepatitis research.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CP-24879 (hydrochloride) 構造式

CAS 番号 : 10141-51-2

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 126	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 126	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$54	在庫あり	Estimated Time of Arrival: December 31
5 mg	$115	在庫あり	Estimated Time of Arrival: December 31
10 mg	$185	在庫あり	Estimated Time of Arrival: December 31
25 mg	$350	在庫あり	Estimated Time of Arrival: December 31
50 mg	$560	在庫あり	Estimated Time of Arrival: December 31
100 mg	$840	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

IC₅₀: 0.015 μM (delta6D in ABMC-7 cells), 0.56 μM (delta6D in Liver microsomes), 0.67 μM (delta5D in ABMC-7 cells), 3.4 μM (delta5D in ABMC-7 cells)^[1]

体外実験

CP-24879 (hydrochloride) (0-10 μM, 4 days) inhibits Δ6 + Δ5 desaturase activities in a concentration-dependent manner, with a concentration-dependent depletion of AA and decrease in LTC₄ production^[1].
CP-24879 (hydrochloride) (0-10 μM, 16 h) shows the inhibitory responses on oleic acid-induced triglyceride accumulation in hepatocytes^[2].
CP-24879 (hydrochloride) (0-10 μM, 16 h) blocks LPS-induced expression of inflammatory cytokines in a concentration-dependent manner^[2].
CP-24879 (hydrochloride) (0-2 μM, 4 h) inhibits desaturase activity and ameliorates ferroptosis^[3].

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

Cell Viability Assay

Cell Line:	Mouse mastocytoma ABMC-7 cells^[1]
Concentration:	0, 100 nM, 300 nM, 1 μM, 3 μM, and 10 μM
Incubation Time:	4 days
Result:	Inhibited Δ6 + Δ5 desaturase activities in a concentration-dependent manner, with a concentration-dependent depletion of AA and decrease in LTC₄ (Leukotriene C₄) production, and did not inhibit either 5-lipoxygenase or LTC₄ synthase activity.

体内実験

CP-24879 (hydrochloride) (3 mg/kg, IP, three times a day, for 6 or 4 days) inhibits Δ6 + Δ5 desaturase activities in vivo, causing depletion of AA in the livers of chow-fed mice and preventing repletion of AA in the livers of EFAD mice^[1].
CP-24879 (hydrochloride) (33 mg/kg, IV, once) is cleared quite rapidly and has a relatively short half-life^[1].

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

Animal Model:	Chow-fed and EFAD Balb/C mice (N = 5/group) ^[1]
Dosage:	3 mg/kg
Administration:	IP, three times a day, for 6 or 4 days
Result:	Inhibited approximately 80% combined Δ6 + Δ5 desaturase activities, causing depletion of AA in the livers of chow-fed mice and preventing repletion of AA in the livers of EFAD mice, and increased OA and LA, with a higher ratio of LA/AA in the livers of mice injected with CP-24879 versus saline (4.70 vs 2.00, Chow-fed mice; 2.46 vs 1.40, EFAD mice; respectively).

Animal Model:	Swiss-Webster mice (male, 25 g) ^[1]
Dosage:	33 mg/kg
Administration:	IV in the tail vein, once (Pharmacokinetic Analysis)
Result:	Was readily distributed to the peripheral tissues, with the volume of distribution (V) of 1.9 mL/g, was cleared quite rapidly (CL = 0.56 mL/min) and had a relatively short half-life (T_1/2 = 59 min).

分子量

215.72

分子式

C₁₁H₁₈ClNO

CAS 番号

10141-51-2

Appearance

Solid

Color

Off-white to light brown

SMILES

NC1=CC=C(OCCC(C)C)C=C1.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 125 mg/mL (579.45 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.6356 mL	23.1782 mL	46.3564 mL
5 mM	0.9271 mL	4.6356 mL	9.2713 mL
10 mM	0.4636 mL	2.3178 mL	4.6356 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 (sealed storage, away from moisture). 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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: ≥ 2.5 mg/mL (11.59 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (9.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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 (sealed storage, away from moisture)

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.

純度とドキュメンテーション

純度: 99.59%

Select Batch:

データシート (277 KB) SDS (393 KB)

COA (244 KB) HNMR (272 KB) LCMS (87 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Obukowicz MG, et al. Identification and characterization of a novel delta6/delta5 fatty acid desaturase inhibitor as a potential anti-inflammatory agent. Biochem Pharmacol. 1998 Apr 1;55(7):1045-58. [Content Brief]

[2]. [2]López-Vicario C, et al. Molecular interplay between Δ5/Δ6 desaturases and long-chain fatty acids in the pathogenesis of non-alcoholic steatohepatitis. Gut. 2014 Feb;63(2):344-55. [Content Brief]

[3]. [3]Lee JY, Nam M, Son HY, et al. Polyunsaturated fatty acid biosynthesis pathway determines ferroptosis sensitivity in gastric cancer. Proc Natl Acad Sci U S A. 2020;117(51):32433-32442. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.6356 mL	23.1782 mL	46.3564 mL	115.8910 mL
	5 mM	0.9271 mL	4.6356 mL	9.2713 mL	23.1782 mL
	10 mM	0.4636 mL	2.3178 mL	4.6356 mL	11.5891 mL
	15 mM	0.3090 mL	1.5452 mL	3.0904 mL	7.7261 mL
	20 mM	0.2318 mL	1.1589 mL	2.3178 mL	5.7945 mL
	25 mM	0.1854 mL	0.9271 mL	1.8543 mL	4.6356 mL
	30 mM	0.1545 mL	0.7726 mL	1.5452 mL	3.8630 mL
	40 mM	0.1159 mL	0.5795 mL	1.1589 mL	2.8973 mL
	50 mM	0.0927 mL	0.4636 mL	0.9271 mL	2.3178 mL
	60 mM	0.0773 mL	0.3863 mL	0.7726 mL	1.9315 mL
	80 mM	0.0579 mL	0.2897 mL	0.5795 mL	1.4486 mL
	100 mM	0.0464 mL	0.2318 mL	0.4636 mL	1.1589 mL