DGAT-1 inhibitor 2
Based on 2 publication(s) in Google Scholar
DGAT-1 inhibitor 2 is an orally active DGAT-1 inhibitor with IC50 values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively. DGAT-1 inhibitor 2 increases ROS concentration, GRP78, and PERK protein abundance. DGAT-1 inhibitor 2 increases SREBF1, CPT1A, and MTTP mRNA in fatty acid-treated cells. DGAT-1 inhibitor 2 improves obesity.
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- Purity : 95.33%
- CAS No.: 942999-61-3
- 화학식: C24H28N4O3
- 분자량:420.50
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DGAT-1 inhibitor 2
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Biological Activity
제품 설명
IC50 & Target
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CPT-1A |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HuTu80 | IC50 |
0.003 μM
Compound: 4
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Inhibition of triacylglycerol synthesis in human HuTu 80 cells after 30 mins
Inhibition of triacylglycerol synthesis in human HuTu 80 cells after 30 mins
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[PMID: 19256504] |
| Sf9 | IC50 |
0.015 μM
Compound: 4
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Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography
Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography
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[PMID: 19256504] |
In Vitro
DGAT-1 inhibitor 2 (0.3 μM; 12 h) increases the mRNA abundance of SREBF1, CPT1A, and MTTP in fatty acid-treated primary calf hepatocytes[1].
DGAT-1 inhibitor 2 (Compound 4) shows potent inhibitory activity against DGAT-1, with IC50 values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively[2].
DGAT-1 inhibitor 2 (Compound 4) exhibits excellent potency in inhibiting Triacylglycerol synthesis in human HuTu 80 cells with an IC50 of 3 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
DGAT-1 inhibitor 2 (Compound 4) (0.3 mg/kg; p.o.) significantly reduces plasma triacylglycerol excursion in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 942999-61-3
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Appearance Solid
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분자량 420.50
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화학식 C24H28N4O3
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Color Light yellow to yellow
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SMILES
O=C(O)CC12CCC(CC1)(CC2)C3=CC=C(C=C3)C4=NC5=C(N)N=CN=C5OC4(C)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Dairy Sci
Diacylglycerol O-acyltransferase (DGAT) isoforms play a role in peridroplet mitochondrial fatty acid metabolism in bovine liver. [Abstract]2024 Nov;107(11):9897-9914. PMID: 38851581 -
J Dairy Sci
Role of diacylglycerol O-acyltransferase (DGAT) isoforms in bovine hepatic fatty acid metabolism. [Abstract]2022 Apr;105(4):3588-3600. PMID: 35181144
용액&용해도
In Vitro:
DMSO : 25 mg/mL (59.45 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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
순도&문서
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Data Sheet (274 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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Handling Instructions (2659 KB)
References
[1]. Yang W, et al. Role of diacylglycerol O-acyltransferase (DGAT) isoforms in bovine hepatic fatty acid metabolism. J Dairy Sci. 2022 Apr;105(4):3588-3600. [Content Brief]
[2]. Birch AM, et al. Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. J Med Chem. 2009 Mar 26;52(6):1558-68. [Content Brief]
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 | 2.3781 mL | 11.8906 mL | 23.7812 mL | 59.4530 mL |
| 5 mM | 0.4756 mL | 2.3781 mL | 4.7562 mL | 11.8906 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3781 mL | 5.9453 mL | |
| 15 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL | 3.9635 mL | |
| 20 mM | 0.1189 mL | 0.5945 mL | 1.1891 mL | 2.9727 mL | |
| 25 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3781 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7927 mL | 1.9818 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1891 mL |
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