Implitapide

• CAT Number: M135115
• CAS Number: 177469-96-4
• Molecular Formula: C35H37N3O2
• Molecular Weight: 531.69
• Purity: ≥95%
• Synonyms: (2S)-2-cyclopentyl-2-[4-[(2,4-dimethylpyrido[2,3-b]indol-9-yl)methyl]phenyl]-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
• InChI: InChI=1S/C35H37N3O2/c1-23-20-24(2)36-34-32(23)29-14-8-9-15-31(29)38(34)21-25-16-18-28(19-17-25)33(27-12-6-7-13-27)35(40)37-30(22-39)26-10-4-3-5-11-26/h3-5,8-11,14-20,27,30,33,39H,6-7,12-13,21-22H2,1-2H3,(H,37,40)/t30-,33-/m0/s1
• InChIKey: KIMRCJZMVARVSU-DITALETJSA-N
• SMILES: CC1=CC(=NC2=C1C3=CC=CC=C3N2CC4=CC=C(C=C4)C(C5CCCC5)C(=O)NC(CO)C6=CC=CC=C6)C

Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.
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].
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].

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.
 [Content Brief]