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ABT-046 CAS: 1031336-60-3

Category: Inhibitors
Product Name: ABT-046
Cat No: I000186
CAS No: 1031336-60-3
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
SMILES: O=C(O)CC1CCC(C2=CC=C(C3=C(N)N4C(N=C3)=CC=N4)C=C2)CC1
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
Solubility: 10 mM in DMSO
Target: DGAT
IC50: 8 nM [1]
Storage: Store at -20°C
CAS 1031336-60-3,ABT-046
  • Description

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.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


[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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