| Bioactivity | ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1[1]. | ||||||||||||
| Target | IC50: 8 nM (hDGAT-1 and mDGAT-1) | ||||||||||||
| Invitro | ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC50 of 78 nM[1].ABT-046 exhibits high in vitro permeability values in Caco-2 cells with no evidence of active efflux (efflux ratio = 1.4 and 1.1 at 0.5 and 5 μM, respectively)[1].ABT-046 demonstrates negligible turnover in microsome preparations from mouse and human livers[1]. | ||||||||||||
| In Vivo | ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice[1].ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion in diet-induced obesity mice[1]. Animal Model: | ||||||||||||
| Name | ABT-046 | ||||||||||||
| CAS | 1031336-60-3 | ||||||||||||
| Formula | C20H22N4O2 | ||||||||||||
| Molar Mass | 350.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Yeh VS, et al. Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of Acyl-CoA: Diacylglycerol acyltransferase 1. J Med Chem. 2012 Feb 23;55(4):1751-1757. |