Avasimibe

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Avasimibe (CI-1011, PD-148515) 是一种有效的选择性酰基辅酶A：胆固醇 O-酰基转移酶 (ACAT) 抑制剂，IC50 为 60 nM。

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.

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.

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.

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

Others

Other Targets

ACAT|CYP1A2|CYP2C19|CYP2C9

Cardiovascular Disease

Dyslipidemia

166518-60-1

501.72102

C29H43NO4S

>98% (HPLC)

DMSO: ≥ 28 mg/mL

c1(C(C)C)cc(cc(c1CC(NS(Oc1c(cccc1C(C)C)C(C)C)(=O)=O)=O)C(C)C)C(C)C

Sulfamic acid, N-[2-[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl)phenyl ester

(-20℃)

With Ice Pack

≥ 2 years