ABT-046

SKU: orb1707729

Description

ABT-046 is a potent and selective oral DGAT-1 inhibitor used in metabolic disease research. It has been employed in studies investigating obesity and type 2 diabetes, demonstrating utility in both in vitro enzymatic assays and in vivo models of metabolic dysfunction.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1031336-60-3
• MW: 350.41
• Purity: 98.13%
• Formula: C₂₀H₂₂N₄O₂
• SMILES: NC1=C(C=NC=2N1N=CC2)C3=CC=C(C=C3)[C@@H]4CC[C@@H](CC(O)=O)CC4
• Target: Transferase,Acyltransferase
• Solubility: DMSO:50 mg/mL (142.69 mM)

Bioactivity

• Target IC50:
  DGAT-1 (human):78 nM
• In Vivo:
  Single gavage administration of ABT-046 (0.03-3 mg/kg) significantly reduced postprandial triglyceride levels in CD-1 mice. Single gavage administration of ABT-046 (0.3 mg/kg) effectively suppressed postprandial triglyceride fluctuations in diet-induced obese mice.
• In Vitro:
  ABT-046 did not significantly inhibit human DGAT-2, but prevented human DGAT-1 from catalyzing triglyceride production in HeLa cells, with an IC50 of 78 nM. In Caco-2 cells, ABT-046 exhibited high in vitro permeability and no active efflux was detected (efflux ratios of 1.4 and 1.1 at 0.5 and 5 μM, respectively). ABT-046 was also found to inhibit human DGAT-2, but prevented human DGAT-1 from catalyzing triglyceride production in HeLa cells with an IC50 of 78 nM. The metabolic conversion of ABT-046 to mouse and human liver microsomes is extremely low and almost negligible.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ABT 046, ABT046, ABT-046

Compound Identifiers

PubChem CID

56933229