DGAT1-IN-3
Based on 1 Customer Validation
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.92%
- CAS. Nr.: 939375-07-2
- Formel: C20H19F3N4O3
- Molecular Weight:420.39
-
Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Orally Active Compound Library
HY-L061
-
Anti-Obesity Compound Library
HY-L087
-
Lipid Metabolism Compound Library
HY-L091
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Metabolism/Protease Compound Library
HY-L012
Biologische Aktivität
IC50: 38 nM (human DGAT-1); 120 nM (rat DGAT-1)[2]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
0.66 μM
Compound: 25
|
Inhibition of human DGAT1 expressed in CHOK1 cells using 14C palmitic acid as substrate after 1 hr by TLC analysis
Inhibition of human DGAT1 expressed in CHOK1 cells using 14C palmitic acid as substrate after 1 hr by TLC analysis
|
[PMID: 22001092] |
| CHO-K1 | EC50 |
0.66 μM
Compound: 6
|
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using [14C]palmitic acid by TLC analysis
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using [14C]palmitic acid by TLC analysis
|
[PMID: 21413799] |
| CHO-K1 | EC50 |
0.661 μM
Compound: 6
|
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay
|
[PMID: 21413799] |
| Sf9 | IC50 |
38 nM
Compound: 5
|
Inhibition of human DGAT1 expressed in Sf9 cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-Co A substrates incubated for 2 hrs by scintillation counting method
Inhibition of human DGAT1 expressed in Sf9 cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-Co A substrates incubated for 2 hrs by scintillation counting method
|
[PMID: 23317570] |
DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM[1].
DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC50 of 0.66 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DGAT1-IN-3 (50 mg/kg; p.o) exhibits good oral bioavailability (77%) and the maximum exposure level in plasma (Cmax) is 24 μM[2].
DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)[2]
-
Dosage:0, 5, 25, 50 mg/kg; once daily for three weeks
-
Administration:P.o. administration
-
Result:Reduced cumulative body weight gain in a dose-dependent manner and was well tolerated in rats.
-
Animal Model:Male Wistar rats[2]
-
Dosage:50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
-
Administration:P.o. and i.v. administration
-
Result:Cmax (24 μM); T1/2 (1.95 h).
Chemical Information
-
CAS. Nr. 939375-07-2
-
Appearance Solid
-
Molecular Weight 420.39
-
Formel C20H19F3N4O3
-
Color Light yellow to yellow
-
SMILES
O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (237.87 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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); 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 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
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)
-
Handling Instructions (2659 KB)
Verweise
[1]. Gómez-Outes A, et al. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59. [Content Brief]
[2]. Yimin Q, et, al. Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem. 2011 Apr 14; 54(7): 2433-46. [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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3787 mL | 11.8937 mL | 23.7874 mL | 59.4686 mL |
| 5 mM | 0.4757 mL | 2.3787 mL | 4.7575 mL | 11.8937 mL | |
| 10 mM | 0.2379 mL | 1.1894 mL | 2.3787 mL | 5.9469 mL | |
| 15 mM | 0.1586 mL | 0.7929 mL | 1.5858 mL | 3.9646 mL | |
| 20 mM | 0.1189 mL | 0.5947 mL | 1.1894 mL | 2.9734 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9515 mL | 2.3787 mL | |
| 30 mM | 0.0793 mL | 0.3965 mL | 0.7929 mL | 1.9823 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5947 mL | 1.4867 mL | |
| 50 mM | 0.0476 mL | 0.2379 mL | 0.4757 mL | 1.1894 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3965 mL | 0.9911 mL | |
| 80 mM | 0.0297 mL | 0.1487 mL | 0.2973 mL | 0.7434 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2379 mL | 0.5947 mL |
DGAT1-IN-3 Related Classifications
HY-16434 Related Classifications
Powered by Bioz