DC260126
Based on 3 publication(s) in Google Scholar
DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.
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- Pureté: 99.57%
- CAS No.: 346692-04-4
- Formule: C16H18FNO2S
- Masse moléculaire:307.38
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Stockage: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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Activité biologique
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) DC260126
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Activité biologique
DC260126 reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 346692-04-4
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Appearance Solid
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Masse moléculaire 307.38
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Formule C16H18FNO2S
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Color White to off-white
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SMILES
O=S(C1=CC=C(F)C=C1)(NC2=CC=C(CCCC)C=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
2024 Jul 19;10(1):329. PMID: 39030174 -
Respir Res
Targeting of G-protein coupled receptor 40 alleviates airway hyperresponsiveness through RhoA/ROCK1 signaling pathway in obese asthmatic mice. [Abstract]2023 Feb 17;24(1):56. PMID: 36803977
DC260126 purchased from MedChemExpress. Usage Cited in: Respir Res. 2023 Feb 17;24(1):56. [Abstract]
The cells were pretreated with 1 μM and 10 μM DC260126 for 0.5 h, then 24 h OA (10 μM)-induced cell proliferation was measured by CCK-8 kit.
DC260126 purchased from MedChemExpress. Usage Cited in: Respir Res. 2023 Feb 17;24(1):56. [Abstract]
Pretreatment with DC260126 at 3 mg/kg or 10 mg/kg to HFD-OVA mice significantly alleviated the inflammatory cell infiltration by H&E staining.
DC260126 purchased from MedChemExpress. Usage Cited in: Respir Res. 2023 Feb 17;24(1):56. [Abstract]
The levels of IL-4, IL-5, and IL-13 in serum were significantly increased in OVA and HFD-OVA mice compared to the control mice, however, these increases were significantly reduced in 10 mg/kg DC260126 treatment group by ELISA.
DC260126 purchased from MedChemExpress. Usage Cited in: Respir Res. 2023 Feb 17;24(1):56. [Abstract]
Pretreatment with DC260126 (10 mg/kg) could significantly reduce IL-1β, TNF-α and elevated IFN-γ expression in the lung tissue of mice by real-time PCR.
DC260126 purchased from MedChemExpress. Usage Cited in: Respir Res. 2023 Feb 17;24(1):56. [Abstract]
The cells were pretreated with 1 μM and 10 μM DC260126 for 0.5 h, the effects of OA (10 µM) on cell cycle were assessed by flow cytometry.
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Pediatr Allergy Immunol
Dispersion and utilization of lipid droplets mediates respiratory syncytial virus-induced airway hyperresponsiveness. [Abstract]2022 Jan;33(1):e13651. PMID: 34383332
Solvant et solubilité
DMSO : ≥ 100 mg/mL (325.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.13 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.
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.
Protocole
Mice[1]
Male C57BL/KsJ-Lepdb (db/db) are maintained in a 12 h light-dark cycle at a temperature of 23°C with free access to water and regular chow diet. To investigate the dose-dependent effect of DC260126, nine-week-old db/db male mice are divided into four groups (n=6/group). Mice are give vehicle (5% DMSO in PBS) or DC260126 (3, 10, 30 mg/kg) once daily by tail vein injection for 5 days. At day 5, each group of mice are fasted for 6 h and blood samples are collected from orbital venous plexus and centrifuged for serum separation. Then the concentration of serum insulin level is measured by ELISA kit. For long term experiments, six-week-old obese db/db male mice are divided into two groups (n=8/group) and given vehicle (5% DMSO in PBS) or DC260126 (10 mg/kg) once daily by tail vein injection for 24 days, respectively.
Rats[2]
Female obese (fa/fa) Zucker rats are maintained in a 12:12 light-dark cycle with free access to water and a high-fat diet containing 15% fat, 1% cholesterol, 0.5% sodium cholate and 15% sucrose, except when fasted before some experiments. Rats at 8 weeks of age are divided into two groups (n=6/group) on the basis of body weight. Rats are injected intraperitoneally once daily with vehicle (propylene glycol) or DC260126 (6 mg/kg) for 8 weeks. Food intake and body weight are monitored periodically. At the end of the experimental period, mice are fasted for 12 h and then blood is collected. Liver, renal, adipose tissues are rapidly excised and weighed. Liver samples are snap frozen in liquid nitrogen and stored at -80°C for western blotting analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Hu H, et al. A novel class of antagonists for the FFAs receptor GPR40. Biochem Biophys Res Commun. 2009;390(3):557-563. [Content Brief]
[2]. Wu J, et al. Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis [published correction appears in J Cell Biochem. 2013 May;114(5):1216]. J Cell Biochem. 2012;113(4):1152-1158. [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 | 3.2533 mL | 16.2665 mL | 32.5330 mL | 81.3326 mL |
| 5 mM | 0.6507 mL | 3.2533 mL | 6.5066 mL | 16.2665 mL | |
| 10 mM | 0.3253 mL | 1.6267 mL | 3.2533 mL | 8.1333 mL | |
| 15 mM | 0.2169 mL | 1.0844 mL | 2.1689 mL | 5.4222 mL | |
| 20 mM | 0.1627 mL | 0.8133 mL | 1.6267 mL | 4.0666 mL | |
| 25 mM | 0.1301 mL | 0.6507 mL | 1.3013 mL | 3.2533 mL | |
| 30 mM | 0.1084 mL | 0.5422 mL | 1.0844 mL | 2.7111 mL | |
| 40 mM | 0.0813 mL | 0.4067 mL | 0.8133 mL | 2.0333 mL | |
| 50 mM | 0.0651 mL | 0.3253 mL | 0.6507 mL | 1.6267 mL | |
| 60 mM | 0.0542 mL | 0.2711 mL | 0.5422 mL | 1.3555 mL | |
| 80 mM | 0.0407 mL | 0.2033 mL | 0.4067 mL | 1.0167 mL | |
| 100 mM | 0.0325 mL | 0.1627 mL | 0.3253 mL | 0.8133 mL |
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