ABT-046


CAS No. : 1031336-60-3

ABT-046,1031336-60-3
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000186
Synonyms:2-((1r,4r)-4-(4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl)cyclohexyl)acetic acid
Molecular Formula:C20H22N4O2
Molecular Weight:350.41
Target:DGAT
IC50:8 nM [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000186
Cas No:1031336-60-3
Product-Name:ABT-046
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:O=C(O)CC1CCC(C2=CC=C(C3=C(N)N4C(N=C3)=CC=N4)C=C2)CC1

ABT-046 is a potent, selective, and orally bioavailable Diacylglycerol acyltransferase 1 (DGAT-1 ) inhibitor (IC50= 8 nM).
IC50 value: 8 nM [1]
Target: DGAT-1
Oral administration at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels, thus culminating in the nomination of 14 as clinical candidate ABT-046.


[1]. Yeh, Vince S. C.; Beno, David W. A.; Brodjian, Sevan 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):1751-7. doi: 10.1021/jm201524g. Epub 2012 Feb 10. Abstract A high-throughput screen against human DGAT-1 led to the identification of a core structure that was subsequently optimized to afford the potent, selective, and orally bioavailable compound 14. Oral administration at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels, thus culminating in the nomination of 14 as clinical candidate ABT-046.

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