| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
DGAT1-IN-1 specifically targets diacylglycerol O-acyltransferase type 1 (DGAT1), an enzyme that catalyzes the final and rate-limiting step in triglyceride synthesis. By inhibiting DGAT1, the compound blocks the esterification of diacylglycerol with fatty acyl-CoA to form triglycerides. This inhibition reduces triglyceride accumulation and modulates lipid metabolism. DGAT1 is a key therapeutic target for conditions such as obesity, type 2 diabetes, and other metabolic disorders.
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| ln Vitro |
In vitro, DGAT1-IN-1 demonstrates potent inhibitory activity against DGAT1. In cell-free assays using lysates of Hep3B cells overexpressing human DGAT1, the compound shows an IC50 of less than 10 nM. This high potency makes it a valuable tool for studying the enzyme's function in lipid metabolism. The compound's activity is confirmed through various biochemical assays that measure the inhibition of DGAT1-mediated triglyceride synthesis.
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| ln Vivo |
In vivo, DGAT1-IN-1 has been studied for its potential to treat diseases modulated by DGAT1 inhibition, such as obesity-related disorders and type 2 diabetes. While specific in vivo efficacy data for this particular compound is limited, DGAT1 inhibitors in general have shown promise in reducing body weight, improving insulin sensitivity, and lowering triglyceride levels in animal models. DGAT1-IN-1 is used in preclinical research to explore these therapeutic applications.
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| Enzyme Assay |
In vitro enzyme assays for DGAT1-IN-1 typically measure its ability to inhibit DGAT1 activity. The enzyme is incubated with its substrates (diacylglycerol and fatty acyl-CoA) in the presence of increasing concentrations of the compound. The formation of triglycerides is then quantified using radiometric or chromatographic methods. IC50 values are calculated from dose-response curves. The compound's potent activity (IC50 < 10 nM) is confirmed using lysates from Hep3B cells overexpressing human DGAT1.
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| Cell Assay |
Cell-based assays for DGAT1-IN-1 involve treating cells that express DGAT1 with the compound and measuring triglyceride synthesis and accumulation. Hep3B cells overexpressing DGAT1 are commonly used. Cells are treated with varying concentrations of the compound, and intracellular triglyceride levels are quantified. The compound's ability to inhibit DGAT1-mediated lipid synthesis is assessed, and its effects on cell viability and metabolism are also evaluated.
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| Animal Protocol |
In vivo animal studies for DGAT1-IN-1 are typically conducted in mouse models of obesity or metabolic syndrome. The compound is administered orally, and its effects on body weight, food intake, serum triglyceride levels, and insulin sensitivity are measured. Tissue samples (e.g., liver, adipose tissue) are collected to assess triglyceride content and gene expression related to lipid metabolism. These studies help evaluate the therapeutic potential of DGAT1 inhibition.
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| ADME/Pharmacokinetics |
DGAT1-IN-1 has a molecular weight of 551.56 g/mol and a molecular formula of C30H28F3N3O4. It has a LogP of 6.92, indicating high lipophilicity. The compound is soluble in DMSO at approximately 20 mg/mL (36.26 mM). For storage, the powder should be kept at -20°C for up to 3 years or at 4°C for up to 2 years; in solution, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound is stable at room temperature for a few days during shipping.
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| Toxicity/Toxicokinetics |
The toxicological profile of DGAT1-IN-1 has not been extensively characterized in public literature. As with any potent enzyme inhibitor, there is potential for off-target effects, and researchers are advised to include appropriate controls in their experiments. The compound is intended for research use only and is not for human or veterinary use.
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| References |
Description: DGAT1-IN-1 is a potent DGAT1 inhibitor. |
| Additional Infomation |
DGAT1-IN-1 is a research compound with no approved human therapeutic use. It is a valuable tool for studying the role of DGAT1 in triglyceride synthesis and lipid metabolism. The compound is used in drug discovery research to explore the potential of DGAT1 inhibition for treating obesity, type 2 diabetes, and related metabolic disorders. It is also used as a reference compound in assays to identify and characterize novel DGAT1 inhibitors.
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| Molecular Formula |
C30H28F3N3O4
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|---|---|
| Molecular Weight |
551.556238174438
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| Exact Mass |
551.203
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| CAS # |
1449779-49-0
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| Related CAS # |
1449779-49-0;
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| PubChem CID |
71696573
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.620
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| LogP |
6.92
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
40
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| Complexity |
850
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=CN4C=C(N=C4C=C3)C(=O)NCC5=CC=C(C=C5)OC(F)(F)F
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| InChi Key |
KFGSQOIWOCDWAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H28F3N3O4/c31-30(32,33)40-25-12-3-20(4-13-25)16-34-29(39)26-18-36-17-24(11-14-27(36)35-26)23-9-7-22(8-10-23)21-5-1-19(2-6-21)15-28(37)38/h3-4,7-14,17-19,21H,1-2,5-6,15-16H2,(H,34,39)(H,37,38)
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| Chemical Name |
2-[4-[4-[2-[[4-(trifluoromethoxy)phenyl]methylcarbamoyl]imidazo[1,2-a]pyridin-6-yl]phenyl]cyclohexyl]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 : ~20 mg/mL (~36.26 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8130 mL | 9.0652 mL | 18.1304 mL | |
| 5 mM | 0.3626 mL | 1.8130 mL | 3.6261 mL | |
| 10 mM | 0.1813 mL | 0.9065 mL | 1.8130 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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