| Bioactivity | Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor. |
| Target | MTP |
| Invitro | Implitapide suppresses MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC50=10 nM) and inhibit secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) with an IC50 value of 1.1 nM[1]. |
| In Vivo | Implitapide (3.2 mg/kg/d) significantly reduces the plasma lipid levels to nearly or below the chow diet (CD) level at 4 and 8 weeks of treatment (p<0.01). Implitapide (3.2 mg/kg/d) markedly suppresses lipid-stained lesions in the mice fed the western-type diet (WD). Implitapide (3.2 mg/kg/d) significantly decreases lesion area by 83% compared with that of the WD group (p<0.01). ApoE KO mice fed a WD containing Implitapide (1, 5, and 15 mg/kg/d) for 14 weeks have been shown to reduce significantly both plaque area (by 66, 78, and 93%, respectively) and lipid moieties within plaque (4.3, 2.6, and 0%, respectively, versus 9.5% in controls). Implitapide at a dosage of approximately 3.2 mg/kg/d significantly reduces the lipid-stained aortic lesions by 83% in apoE KO mice[1]. |
| Name | Implitapide |
| CAS | 177469-96-4 |
| Formula | C35H37N3O2 |
| Molar Mass | 531.69 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Ueshima K, et al. Implitapide, a microsomal triglyceride transfer protein inhibitor, reduces progression of atherosclerosis in apolipoprotein E knockout mice fed a Western-type diet: involvement of the inhibition of postprandial triglyceride elevation. Biol Pharm Bull. 2005 Feb;28(2):247-52. |