ABT-046

• CAT Number: I000186
• CAS Number: 1031336-60-3
• Molecular Formula: C20H22N4O2
• Molecular Weight: 350.41
• Purity: ≥95%
• Synonyms: 2-[4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl]acetic acid
• InChI: InChI=1S/C20H22N4O2/c21-20-17(12-22-18-9-10-23-24(18)20)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-19(25)26/h5-10,12-14H,1-4,11,21H2,(H,25,26)
• InChIKey: BWUXSHHOKODNAK-UHFFFAOYSA-N
• SMILES: C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=C(N4C(=CC=N4)N=C3)N

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].
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].
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].

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.
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