| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
DGAT-1 inhibitor 2 targets DGAT-1 (acyl-CoA:diacylglycerol acyltransferase 1), an enzyme that catalyzes the final step of triglyceride synthesis. By inhibiting DGAT-1, the compound reduces triglyceride synthesis and fat absorption. This mechanism makes it a potential therapeutic target for obesity and metabolic diseases.
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| ln Vitro |
In vitro, DGAT-1 inhibitor 2 acts as an effective inhibitor of DGAT-1 activity. Its activity is assessed using enzyme inhibition assays with purified DGAT-1 enzyme and radiolabeled substrates. The compound's potency is measured by determining the IC₅₀ value for DGAT-1 inhibition. It is also evaluated in cellular models of lipid metabolism.
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| ln Vivo |
In vivo, DGAT-1 inhibitor 2 exhibits weight loss effects. As an anti-obesity agent, it reduces fat absorption and triglyceride synthesis. The compound is used as a pharmacological tool to validate DGAT-1 as a therapeutic target for metabolic diseases. Further in vivo studies are needed to fully characterize its efficacy and safety.
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| Enzyme Assay |
In vitro enzyme inhibition assays for DGAT-1 inhibitor 2 are performed using purified DGAT-1 enzyme. The enzyme is incubated with acyl-CoA and diacylglycerol substrates in the presence of increasing concentrations of the compound. The incorporation of radiolabeled acyl-CoA into triglycerides is measured, and the IC₅₀ is calculated from the inhibition curve.
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| Cell Assay |
In vitro cellular assays for DGAT-1 inhibitor 2 are performed using hepatocytes or intestinal cells. Cells are treated with the compound, and triglyceride synthesis is measured by incorporation of radiolabeled fatty acids. Lipid accumulation is assessed by oil red O staining or other lipid quantification methods. These assays characterize the compound's effects on cellular lipid metabolism.
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| Animal Protocol |
In vivo animal experiments for DGAT-1 inhibitor 2 are conducted in rodent models of obesity. A typical protocol involves oral administration of the compound to diet-induced obese mice, followed by measurement of body weight, food intake, and fat mass. Metabolic parameters such as glucose tolerance, insulin sensitivity, and lipid profiles are also assessed to evaluate the compound's anti-obesity effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DGAT-1 inhibitor 2 have not been fully characterized. The compound has a molecular weight of 420.50 and molecular formula C₂₄H₂₈N₄O₃. It is soluble in DMSO at 25 mg/mL. It should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Toxicological data for DGAT-1 inhibitor 2 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
DGAT-1 inhibitor 2 is a potent DGAT-1 inhibitor with CAS number 942999-61-3, molecular formula C₂₄H₂₈N₄O₃, and molecular weight 420.50. It inhibits DGAT-1, the enzyme that catalyzes the final step of triglyceride synthesis, and exhibits weight loss effects. It is used in lipid metabolism and obesity research. This product is for research use only.
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| Molecular Formula |
C24H28N4O3
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|---|---|
| Molecular Weight |
420.50412
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| Exact Mass |
420.216
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| CAS # |
942999-61-3
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| PubChem CID |
16202164
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.434
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
719
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VGPKUACRBMPJLF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28N4O3/c1-22(2)19(28-18-20(25)26-14-27-21(18)31-22)15-3-5-16(6-4-15)24-10-7-23(8-11-24,9-12-24)13-17(29)30/h3-6,14H,7-13H2,1-2H3,(H,29,30)(H2,25,26,27)
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| Chemical Name |
2-[4-[4-(4-amino-7,7-dimethylpyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-1-bicyclo[2.2.2]octanyl]acetic acid
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| HS Tariff Code |
2934.99.9001
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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 : ~25 mg/mL (~59.45 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.95 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3781 mL | 11.8906 mL | 23.7812 mL | |
| 5 mM | 0.4756 mL | 2.3781 mL | 4.7562 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3781 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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