| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T46628 | ||||
| Target Name | Microsomal triglyceride transfer protein (MTTP) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | BMS-201038 | Drug Info | IC50 = 8 nM | [3] | |
| DIRLOTAPIDE | Drug Info | IC50 = 2.9 nM | [1] | ||
| Action against Disease Model | Implitapide | Drug Info | Implitapide was shown to suppress MTP activity using a recombinant h uMan form complexed with protein disulphide isomerase(IC50=10 nM )and inhibit secretion of apoB-containing VLDL-like lipoproteins from a h uMan hepatoma cell(HepG2) with an IC 50 value of 1.1 nM. | [2] | |
| References | |||||
| REF 1 | In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlota... Bioorg Med Chem Lett. 2007 Apr 1;17(7):1996-9. | ||||
| REF 2 | 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. | ||||
| REF 3 | 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. | ||||
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