Avasimibe

SKU: orb1225989

Description

Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM; potently reduces plasma cholesterol in chow-fed rats and in rabbits fed a cholesterol-free, casein-containing diet characterized by both hepatic overproduction of apo B-containing lipoproteins and delayed lipoprotein clearance; decreases both VLDL and LDL apolipoprotein B production in miniature pigs; synergistically reduces cholesteryl ester content in THP-1 macrophages combined with Atorvastatin,Dyslipidemia Phase 3 Discontinued.

Key Properties

• CAS Number: 166518-60-1
• MW: 501.72102
• Purity: >98% (HPLC)
• Formula: C₂₉H₄₃NO₄S
• SMILES: c1(C(C)C)cc(cc(c1CC(NS(Oc1c(cccc1C(C)C)C(C)C)(=O)=O)=O)C(C)C)C(C)C
• Target: ACAT|CYP1A2|CYP2C19|CYP2C9
• Solubility: DMSO: ≥ 28 mg/mL

Bioactivity

• In Vivo:
  Animal model: SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells. Dosage: 30 mg/kg. Administration: Intraperitoneally injected for 7 weeks. Result: Reduced tumour volume compared with that of the control group. Inhibited PCa growth and migration In vivo.
• In Vitro:
  Cell Viability Assay Cell line: PCa cells (PC-3 and DU 145). Concentration: 0, 0.25, 5, 10, 20, 40 and 80 μM Incubation time: 1, 2, and 3 days. Result: Dose dependently inhibited PC-3 and DU 145 cell viability. Western blot analysis. Cell line: PCa cells (PC-3 and DU 145). Concentration: 10 and 20 μM. Incubation time: 48 hours. Result: Reduced protein levels of EMT-related proteins (β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin). Cell Cycle Analysis Cell line: PCa cells (PC-3 and DU 145). Concentration: 10 and 20 μM. Incubation time: 48 hours. Result: Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CI-1011 | PD-148515 | CI1011 | PD148515 | CI 1011 | PD 148515

Quick Database Links

Gene Symbol

ACAT|CYP1A2|CYP2C19|CYP2C9