DGAT1-IN-3 |
| Catalog No.GC60134 |
DGAT1-IN-3 est un inhibiteur puissant, sélectif et biodisponible par voie orale de DGAT-1, avec des IC50 de 38 nM pour la DGAT-1 humaine et de 120 nM pour la DGAT-1 de rat.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 939375-07-2
Sample solution is provided at 25 µL, 10mM.
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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[1][2].
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].
DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile[2].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]. Animal Model: Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)[2]
[1]. 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. [2]. Weiya Y, et, al. Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors. Bioorg Med Chem Lett. 2011 Dec 1; 21(23): 7205-9.
| Cas No. | 939375-07-2 | SDF | |
| Canonical SMILES | O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3 | ||
| Formula | C20H19F3N4O3 | M.Wt | 420.39 |
| Solubility | DMSO: 100 mg/mL (237.87 mM) | Storage | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3787 mL | 11.8937 mL | 23.7874 mL |
| 5 mM | 0.4757 mL | 2.3787 mL | 4.7575 mL |
| 10 mM | 0.2379 mL | 1.1894 mL | 2.3787 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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