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Purity: ≥98%
ABT-046 is a novel, potent, selective, and orally bioavailableinhibitor of diacylglycerol acyltransferase 1 (DGAT-1 ) with IC50 of 8 nM. It was identified from a high-throughput screen against human 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.
| ln Vitro |
ABT-046 can prevent the synthesis of triglycerides in HeLa cells that express human DGAT-1 with an IC50 of 78 nM, however it has no inhibitory impact on human DGAT-2[1]. When tested in Caco-2 cells, ABT-046 had high in vitro permeability values but no sign of active efflux (efflux ratios of 1.4 and 1.1 at 0.5 and 5 μM, respectively) [1]. In microsomal preparations from mouse and human livers, ABT-046 has very little turnover [1].
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| ln Vivo |
In CD-1 mice, ABT-046 (0.03-3 mg/kg; ig; once) dramatically lowers postprandial triglycerides [1]. In diet-induced obese mice, ABT-046 (0.3 mg/kg; ir; once) eliminates postprandial triglyceride fluctuations [1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J diet-induced obesity (DIO) mice [1]
Doses: 0.3 mg/kg Route of Administration: po (oral gavage), single dose Experimental Results: Serum triglyceride concentration continued to decrease throughout the experiment. Animal/Disease Models: CD-1 mice and SD (SD (Sprague-Dawley)) rats [1] Doses: 10 mg/kg or 5 mg/kg Route of Administration: intravenous (iv) (iv)injection or po (oral gavage) (pharmacokinetic/PK/PK analysis) Experimental Results: ABT-046a [1] Selected pharmacokinetic/PK/PK properties in mouse (10 mg/kg) Rat (5 mg/kg) ivb T1/2 (h) 4.6 3.8 Vss (L/kg) 0.3 0.3 Clp (L/h/ kg) 0.1 0.05 pob T1/2 (h) 5.1 5.6 Cmax (μg/mL) 17.4 9.3 AUC (μg·h/mL) 151 130 F (%) 78 91 a All values are mean ± SEM (unless otherwise Note, n = 3). b 1% Tween-80 aqueous solution. |
| References |
[1]. Yeh VS, 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):1751-1757.
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| Molecular Formula |
C20H22N4O2
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|---|---|
| Molecular Weight |
350.41428
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| CAS # |
1031336-60-3
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| SMILES |
O=C(O)CC1CCC(C2=CC=C(C3=C(N)N4C(N=C3)=CC=N4)C=C2)CC1
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| InChi Key |
BWUXSHHOKODNAK-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl]acetic acid
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| Synonyms |
ABT-046; ABT 046; ABT046.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~190.26 mM)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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