Description
Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.
Product information
CAS Number: 177469-96-4
Molecular Weight: 531.69
Formula: C35H37N3O2
Chemical Name: 2-cyclopentyl-2-[4-({2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl}methyl)phenyl]-N-(2-hydroxy-1-phenylethyl)acetamide
Smiles: CC1C=C(C)N=C2C=1C1=CC=CC=C1N2CC1C=CC(=CC=1)C(C1CCCC1)C(=O)NC(CO)C1C=CC=CC=1
InChiKey: KIMRCJZMVARVSU-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
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.
Products are for research use only. Not for human use.
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