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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.57%
- CAS 番号: 346692-04-4
- 分子式: C16H18FNO2S
- 分子量:307.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 DC260126
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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ELISA
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RT-PCR
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Flow Cytometry
生物活性
製品説明
体外実験
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. Further protocols information, click here.
化学情報
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CAS 番号 346692-04-4
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性状 Solid
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分子量 307.38
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
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.
プロトコル
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |