ABT-046DGAT-1 inhibitor,potent and selective CAS# 1031336-60-3 |
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Quality Control & MSDS
3D structure
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Number of papers citing our products
| Cas No. | 1031336-60-3 | SDF | Download SDF |
| PubChem ID | 56933229 | Appearance | Powder |
| Formula | C20H22N4O2 | M.Wt | 350.41 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | DGAT-1 inhibitor | ||
| Solubility | DMSO : 66.67 mg/mL (190.26 mM; Need ultrasonic) | ||
| Chemical Name | 2-[4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl]acetic acid | ||
| SMILES | C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=C(N4C(=CC=N4)N=C3)N | ||
| Standard InChIKey | BWUXSHHOKODNAK-UHFFFAOYSA-N | ||
| Standard 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| 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. References: | |||||
ABT-046 Dilution Calculator
ABT-046 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8538 mL | 14.269 mL | 28.538 mL | 57.076 mL | 71.345 mL |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | 11.4152 mL | 14.269 mL |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL | 5.7076 mL | 7.1345 mL |
| 50 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.1415 mL | 1.4269 mL |
| 100 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.5708 mL | 0.7134 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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. [1].
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.
Clinical trial: ABT-046 is currently in the preclinical developlent stage and no clinical data are available.
Reference:
[1] Yeh VS, Beno DW, Brodjian S, Brune ME, Cullen SC, Dayton BD, Dhaon MK, Falls HD, Gao J, Grihalde N, Hajduk P, Hansen TM, Judd AS, King AJ, Klix RC, Larson KJ, Lau YY, Marsh KC, Mittelstadt SW, Plata D, Rozema MJ, Segreti JA, Stoner EJ, Voorbach MJ, Wang X, Xin X, Zhao G, Collins CA, Cox BF, Reilly RM, Kym PR, Souers AJ. Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1. J Med Chem. 2012;55(4):1751-7.
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Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.[Pubmed:22263872]
J Med Chem. 2012 Feb 23;55(4):1751-7.
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.
