ABT-046
Based on 1 Customer Validation
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.57%
- No. CAS: 1031336-60-3
- Fòrmula: C20H22N4O2
- Peso molecular:350.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 8 nM (hDGAT-1 and mDGAT-1)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
78 nM
Compound: 14
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Inhibition of human DGAT1 expressed in human HeLa cells assessed as reduction in triglyceride synthesis
Inhibition of human DGAT1 expressed in human HeLa cells assessed as reduction in triglyceride synthesis
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[PMID: 22263872] |
In Vitro
ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC50 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion in diet-induced obesity mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD-1 mice, postprandial hyperlipidemia model[1]
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Dosage:0.03, 0.3, or 3 mg/kg
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Administration:Oral gavage, single dose
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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 (C2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively).
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Animal Model:Male C57BL/6J diet-induced obesity (DIO) mice[1]
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Dosage:0.3 mg/kg
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Administration:Oral gavage, single dose
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Result:Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.
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Animal Model:CD-1 mice and Sprague-Dawley rats[1]
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Dosage:10 mg/kg or 5 mg/kg
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Administration:Intravenous injection or oral gavage (Pharmacokinetic Analysis)
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Result:Selected Pharmacokinetic Properties of ABT-046a[1]
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 values ± SEMs (n = 3 unless specified otherwise).
b 1% Tween-80 in water.
Chemical Information
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No. CAS 1031336-60-3
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Appearance Solid
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Peso molecular 350.41
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Fòrmula C20H22N4O2
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Color White to off-white
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SMILES
NC1=C(C2=CC=C([C@H]3CC[C@H](CC(O)=O)CC3)C=C2)C=NC4=CC=NN41
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : 66.67 mg/mL (190.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (4.77 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8538 mL | 14.2690 mL | 28.5380 mL | 71.3450 mL |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | 14.2690 mL | |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL | 7.1345 mL | |
| 15 mM | 0.1903 mL | 0.9513 mL | 1.9025 mL | 4.7563 mL | |
| 20 mM | 0.1427 mL | 0.7134 mL | 1.4269 mL | 3.5672 mL | |
| 25 mM | 0.1142 mL | 0.5708 mL | 1.1415 mL | 2.8538 mL | |
| 30 mM | 0.0951 mL | 0.4756 mL | 0.9513 mL | 2.3782 mL | |
| 40 mM | 0.0713 mL | 0.3567 mL | 0.7134 mL | 1.7836 mL | |
| 50 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4269 mL | |
| 60 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1891 mL | |
| 80 mM | 0.0357 mL | 0.1784 mL | 0.3567 mL | 0.8918 mL | |
| 100 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7134 mL |
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