| Identification | Back Directory | [Name]
Pactimibe | [CAS]
189198-30-9 | [Synonyms]
PactiMib
pactimibe
2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo l-5-yl]acetic acid
7-[(2,2-Dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-1H-indole-5-acetic acid | [Molecular Formula]
C25H40N2O3 | [MDL Number]
MFCD11973650 | [MOL File]
189198-30-9.mol | [Molecular Weight]
416.6 |
| Chemical Properties | Back Directory | [Boiling point ]
604.4±55.0 °C(Predicted) | [density ]
1.071 | [storage temp. ]
4°C, away from moisture | [solubility ]
DMSO: 200 mg/mL (480.08 mM) | [form ]
Solid | [pka]
4.00±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | 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 |
| [IC 50]
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) | [References]
[1] Naoki Terasaka, et al. ACAT inhibitor pactimibe sulfate (CS-505) reduces and stabilizes atherosclerotic lesions by cholesterol-lowering and direct effects in apolipoprotein E-deficient mice. Atherosclerosis. 2007 Feb;190(2):239-47. DOI:10.1016/j.atherosclerosis.2006.03.007
[2] Ken Kitayama, et al. Importance of acyl-coenzyme A:cholesterol acyltransferase 1/2 dual inhibition for anti-atherosclerotic potency of pactimibe. Eur J Pharmacol. 2006 Jul 1;540(1-3):121-30. DOI:10.1016/j.ejphar.2006.04.022
[3] Yasunobu Yoshinaka, et al. A selective ACAT-1 inhibitor, K-604, stimulates collagen production in cultured smooth muscle cells and alters plaque phenotype in apolipoprotein E-knockout mice. Atherosclerosis. 2010 Nov;213(1):85-91. DOI:10.1016/j.atherosclerosis.2010.08.048 |
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