シグリタゾン
Based on 1 publication(s) in Google Scholar
Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells.
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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: 99.74%
- CAS 番号: 74772-77-3
- 分子式: C18H23NO3S
- 分子量:333.45
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Ciglitazone
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
3 μM
Compound: 3
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In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
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[PMID: 8576907] |
| HepG2 | EC50 |
10 μM
Compound: Ciglitazone
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
14.1 μM
Compound: Ciglitazone
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| LNCaP | IC50 |
60 μM
Compound: 1, Ciglitazone
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Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay in presence of 10% FBS
Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay in presence of 10% FBS
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[PMID: 22468970] |
| LNCaP | IC50 |
78 μM
Compound: 1, Ciglitazone
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Inhibition of glucose transporter in human LNCAP cells assessed as blocking of [3H]-2-DG uptake after 30 mins by scintillation counting
Inhibition of glucose transporter in human LNCAP cells assessed as blocking of [3H]-2-DG uptake after 30 mins by scintillation counting
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[PMID: 22468970] |
| NIH3T3 | EC50 |
14.9 μM
Compound: ciglitazone
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Agonist activity at human PPARgamma expressed in mouse NIH/3T3 cells assessed as receptor activation after 16 hrs by luciferase based reporter gene assay
Agonist activity at human PPARgamma expressed in mouse NIH/3T3 cells assessed as receptor activation after 16 hrs by luciferase based reporter gene assay
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[PMID: 11975517] |
| PC-12 | IC50 |
20 μM
Compound: Ciglitazone
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Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay
Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay
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[PMID: 15109648] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 74772-77-3
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性状 Solid
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分子量 333.45
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分子式 C18H23NO3S
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Color White to off-white
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SMILES
O=C(N1)SC(CC2=CC=C(OCC3(C)CCCCC3)C=C2)C1=O
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別名
Ciglitazone; ADD-3878; U-63287
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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 (1)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
Macrophage P2Y6R activation aggravates psoriatic inflammation through IL-27-mediated Th1 responses. [Abstract]2024 Oct;14(10):4360-4377. PMID: 39525587
溶剤 & 溶解度
DMSO : 100 mg/mL (299.89 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (7.50 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.50 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.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
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- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996;39(3):665-668. [Content Brief]
[2]. Kim DH, et al. Ciglitazone, a peroxisome proliferator-activated receptor gamma ligand, inhibits proliferation and differentiation of th17 cells. Biomol Ther (Seoul). 2015;23(1):71-76. [Content Brief]
[3]. Chang AY, et al. Ciglitazone, a new hypoglycemic agent. I. Studies in ob/ob and db/db mice, diabetic Chinese hamsters, and normal and streptozotocin-diabetic rats. Diabetes. 1983;32(9):830-838. [Content Brief]
[4]. Kwon CH, et al. Ciglitazone induces apoptosis via activation of p38 MAPK and AIF nuclear translocation mediated by reactive oxygen species and Ca(2+) in opossum kidney cells. Toxicology. 2009;257(1-2):1-9. [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 | 2.9989 mL | 14.9946 mL | 29.9892 mL | 74.9731 mL |
| 5 mM | 0.5998 mL | 2.9989 mL | 5.9978 mL | 14.9946 mL | |
| 10 mM | 0.2999 mL | 1.4995 mL | 2.9989 mL | 7.4973 mL | |
| 15 mM | 0.1999 mL | 0.9996 mL | 1.9993 mL | 4.9982 mL | |
| 20 mM | 0.1499 mL | 0.7497 mL | 1.4995 mL | 3.7487 mL | |
| 25 mM | 0.1200 mL | 0.5998 mL | 1.1996 mL | 2.9989 mL | |
| 30 mM | 0.1000 mL | 0.4998 mL | 0.9996 mL | 2.4991 mL | |
| 40 mM | 0.0750 mL | 0.3749 mL | 0.7497 mL | 1.8743 mL | |
| 50 mM | 0.0600 mL | 0.2999 mL | 0.5998 mL | 1.4995 mL | |
| 60 mM | 0.0500 mL | 0.2499 mL | 0.4998 mL | 1.2496 mL | |
| 80 mM | 0.0375 mL | 0.1874 mL | 0.3749 mL | 0.9372 mL | |
| 100 mM | 0.0300 mL | 0.1499 mL | 0.2999 mL | 0.7497 mL |
Ciglitazone 関連分類
HY-W011220 関連分類
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