2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. Pactimibe

Pactimibe  (Synonyms: CS-505 free base)

製品番号: HY-100401 純度: 99.98%
COA 取扱説明書 Technical Support

Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.

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Pactimibe

Pactimibe 構造式

CAS 番号 : 189198-30-9

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 495 在庫あり
Solution
10 mM * 1 mL in DMSO USD 495 在庫あり
Solid
5 mg $450 在庫あり
10 mg $800 在庫あり
25 mg $1650 在庫あり
50 mg $2550 在庫あり
100 mg $3800 在庫あり
200 mg   お問い合わせ  
500 mg   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

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Pactimibe 関連抗体

Top Publications Citing Use of Products

Acyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

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  • 純度とドキュメンテーション

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製品説明

Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively[1]. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity[2].

IC50 & Target[1][2]

ACAT1

4.9 μM (IC50)

ACAT2

3.0 μM (IC50)

ACAT

2 μM (IC50, in the liver)

ACAT

2.7 μM (IC50, in macrophages)

ACAT

4.7 μM (IC50, in THP-1 cells)

oleoyl-CoA

5.6 μM (Ki)

cholesteryl ester formation

6.7 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
THP-1 IC50
0.3 μM
Compound: 2, pactimibe
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL after differentiation assessed as effect on foam cell formation
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL after differentiation assessed as effect on foam cell formation
[PMID: 18620381]
THP-1 IC50
1.8 μM
Compound: 2, pactimibe
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation
[PMID: 18620381]
THP-1 IC50
2 μM
Compound: 94
Inhibition of accumulation of esterified cholesterol in human THP-1 cells
Inhibition of accumulation of esterified cholesterol in human THP-1 cells
[PMID: 36473091]
体外実験

Pactimibe (CS-505 free base) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation[2].

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

Pactimibe 関連抗体
体内実験

Pactimibe (CS-505 free base; 60 and 200 mg/kg/day; oral gavage; twice a day; 12 weeks) induces an inhibition for ACAT-1 and ACAT-2, causing a reduction of plasma cholesterol but no influence on macrophage- or collagen-positive areas[3].

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

Animal Model: Male C57BL/6J ApoE−/− mice aged 8-week-old[3]
Dosage: 60 and 200 mg/kg/day
Administration: Oral gavage; twice a day; 12 weeks
Result: Decreased plasma cholesterol levels by 39% and 74% at the administration of 60 and 200 mg/kg/day
臨床実験
分子量

416.60

分子式

C25H40N2O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=C(C)C2=C(N(CCCCCCCC)CC2)C(NC(C(C)(C)C)=O)=C1C
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 : 200 mg/mL (480.08 mM; Need ultrasonic; 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 2.4004 mL 12.0019 mL 24.0038 mL
5 mM 0.4801 mL 2.4004 mL 4.8008 mL
10 mM 0.2400 mL 1.2002 mL 2.4004 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

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: ≥ 5 mg/mL (12.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:

Dosage

mg/kg

Animal weight
(per animal)

g

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
参考文献

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4004 mL 12.0019 mL 24.0038 mL 60.0096 mL
5 mM 0.4801 mL 2.4004 mL 4.8008 mL 12.0019 mL
10 mM 0.2400 mL 1.2002 mL 2.4004 mL 6.0010 mL
15 mM 0.1600 mL 0.8001 mL 1.6003 mL 4.0006 mL
20 mM 0.1200 mL 0.6001 mL 1.2002 mL 3.0005 mL
25 mM 0.0960 mL 0.4801 mL 0.9602 mL 2.4004 mL
30 mM 0.0800 mL 0.4001 mL 0.8001 mL 2.0003 mL
40 mM 0.0600 mL 0.3000 mL 0.6001 mL 1.5002 mL
50 mM 0.0480 mL 0.2400 mL 0.4801 mL 1.2002 mL
60 mM 0.0400 mL 0.2000 mL 0.4001 mL 1.0002 mL
80 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7501 mL
100 mM 0.0240 mL 0.1200 mL 0.2400 mL 0.6001 mL
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Pactimibe Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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）
× = ×
C1   V1   C2   V2
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:

Pactimibe189198-30-9CS-505CS505CS 505AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseacyl-CoAatherosclerosishypercholesterolemiaInhibitorinhibitorinhibit

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