Avasimibe

CAS No. 166518-60-1

Avasimibe( CI-1011 | PD-148515 | CI1011 | PD148515 | CI 1011 | PD 148515 )

Catalog No. M12538 CAS No. 166518-60-1

Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
10MG 39 In Stock
25MG 74 In Stock
50MG 133 In Stock
100MG 237 In Stock
200MG 383 In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    Avasimibe
  • Note
    Research use only, not for human use.
  • Brief Description
    Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM.
  • 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.
  • In Vitro
    Cell Viability AssayCell Line:PCa cells (PC-3 and DU 145)Concentration:0, 0.25, 5, 10, 20, 40 and 80 μMIncubation 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.
  • 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.
  • Synonyms
    CI-1011 | PD-148515 | CI1011 | PD148515 | CI 1011 | PD 148515
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    ACAT|CYP1A2|CYP2C19|CYP2C9
  • Research Area
    Cardiovascular Disease
  • Indication
    Dyslipidemia

Chemical Information

  • CAS Number
    166518-60-1
  • Formula Weight
    501.72102
  • Molecular Formula
    C29H43NO4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 28 mg/mL
  • 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
  • Chemical Name
    Sulfamic acid, N-[2-[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl)phenyl ester

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Lee HT, et al. J Med Chem. 1996 Dec 20;39(26):5031-4. 2. Ramharack R, et al. Atherosclerosis. 1998 Jan;136(1):79-87. 3. Burnett JR, et al. J Lipid Res. 1999 Jul;40(7):1317-27. 4. Llaverías G, et al. Eur J Pharmacol. 2002 Sep 6;451(1):11-7.
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