[CAS NO. 1031336-60-3] ABT-046
PRODUCTS SPECIFICATIONS [1031336-60-3]
DESCRIPTION [1031336-60-3]
Overview
| MDL | MFCD22124521 |
|---|---|
| Molecular Weight | 350.41 |
| Molecular Formula | C20H22N4O2 |
| SMILES | NC1=C(C2=CC=C([C@H]3CC[C@H](CC(O)=O)CC3)C=C2)C=NC4=CC=NN41 |
Summary
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 ( DGAT-1 ) inhibitor with IC 50 s of both 8 nM against human and mouse DGAT-1 [1] .
IC50 & Target
IC 50 : 8 nM (hDGAT-1 and mDGAT-1) [1]
In Vitro
ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male CD-1 mice, postprandial hyperlipidemia model [1] |
| Dosage: | 0.03, 0.3, or 3 mg/kg |
| Administration: | Oral gavage, single dose |
| Result: | Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C 2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively). |
| Animal Model: | Male C57BL/6J diet-induced obesity (DIO) mice [1] |
| Dosage: | 0.3 mg/kg |
| Administration: | Oral gavage, single dose |
| Result: | Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment. |
| Animal Model: | CD-1 mice and Sprague-Dawley rats [1] | ||||||||||||||||||||||||||||||
| Dosage: | 10 mg/kg or 5 mg/kg | ||||||||||||||||||||||||||||||
| Administration: | Intravenous injection or oral gavage (Pharmacokinetic Analysis) | ||||||||||||||||||||||||||||||
| Result: |
Selected Pharmacokinetic Properties of ABT-046
a
[1]
a All values are mean values ± SEMs (n = 3 unless specified otherwise). b 1% Tween-80 in water. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 66.67 mg/mL ( 190.26 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8538 mL | 14.2690 mL | 28.5380 mL |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL |
