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

Pactimibe (Synonyms: CS-505 free base)

Cat. No.: HY-100401
Handling Instructions

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.

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

Pactimibe Chemical Structure

Pactimibe Chemical Structure

CAS No. : 189198-30-9

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Description

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)

In Vitro

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

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

In Vivo

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].

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
Molecular Weight

416.60

Formula

C₂₅H₄₀N₂O₃

CAS No.

189198-30-9

SMILES

O=C(O)CC1=C(C)C2=C(N(CCCCCCCC)CC2)C(NC(C(C)(C)C)=O)=C1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PactimibeCS-505CS505CS 505AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseacyl-CoAatherosclerosishypercholesterolemiaInhibitorinhibitorinhibit

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Pactimibe
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