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ABT-046
Cat No.
CEI-1198
Product Overview
The final and only committed step in the synthesis of triglycerides is common to both major triglyceride biosynthesis pathways and is catalyzed by acyl CoA:diacylglycerol acyltransferase (DGAT) enzymes. DGAT-1, in particular, has received significant attention as a therapeutic target for cardiometabolic diseases. 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 ABT-046.
CAS No.
1031336-60-3
Molecular Weight
350.41
Storage
Store at -20°C
Synonyms
DGAT-1 inhibitor; ABT 046; ABT046
Targets
DGAT-1
Molecular Formula
C20H22N4O2
Chemical Name
2-[4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl]acetic acid
Solubility
DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
ABT-046 showed potent inhibition against both human and mouse isoforms of DGAT-1 (IC50 = 8 nM) and retained much of the high BE (BE = 23.1). Additionally, this compound showed no inhibition against human DGAT-2 and inhibited triglyceride formation in HeLa cells expressing human DGAT-1 with an IC50 of 78 nM.
In vivo
Oral administration of ABT-046 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.
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