MCC-555 (Synonyms: Isaglitazone,Netoglitazone,RWJ 241947) |
| カタログ番号GC14595 |
MCC-555 は、PPARα のデュアル アゴニストです。およびPPARγ血糖降下作用があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 161600-01-7
Sample solution is provided at 25 µL, 10mM.
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MCC-555, also known as RWJ-241947, is a novel peroxisome proliferator–activated receptor γ ligand [1].
The PPARγ receptors mainly express in adipose tissue, colon and macrophages involved in regulating fatty acid storage and glucose metabolism. It has been identified that PPARγ is the major functional receptor for the thiazolidinedione class of insulin-sensitizing drugs. The PPARγ receptor is implicated in the processes of adipogenesis and systemic insulin action [2].
MCC-555 (5 μmol/L) exhibited an apoptotic activity in human colorectal cancer cells. MCC-555 significantly increased NAG-1 expression in a PPARγ-independent manner. In HCT-116 cells, treatment with MCC-555 induced apoptosis. MCC-555 affected NAG-1 mRNA stability. MCC-555 treatment induced rapid phosphorylation of ERK1/2 [1]. In various solid and hematological tumor cell lines, MCC-555 showed antiproliferative activity against prostate cancer cells, with the strongest effect against the androgen-independent PC-3 prostate cancer cells [2].
In male beige/nude/X-linked immunodeficient (BNX) mice, treatment with MCC-555 profoundly suppressed growth of PC-3 prostate cancer xenografts with prominent apoptosis, fibrosis, and inflammatory and giant cell reaction. The experimented mice showed significantly decreased cholesterol [3].
References:
[1] Yamaguchi K, Lee S H, Eling T E, et al. A novel peroxisome proliferator–activated receptor γ ligand, MCC-555, induces apoptosis via posttranscriptional regulation of NAG-1 in colorectal cancer cells[J]. Molecular cancer therapeutics, 2006, 5(5): 1352-1361.
[2] Spiegelman B M. PPAR-gamma: adipogenic regulator and thiazolidinedione receptor[J]. Diabetes, 1998, 47(4): 507-514.
[3] Kumagai T, Ikezoe T, Gui D, et al. RWJ-241947 (MCC-555), a unique peroxisome proliferator-activated receptor-γ ligand with antitumor activity against human prostate cancer in vitro and in beige/nude/X-linked immunodeficient mice and enhancement of apoptosis in myeloma cells induced by arsenic trioxide[J]. Clinical Cancer Research, 2004, 10(4): 1508-1520.
| Cas No. | 161600-01-7 | SDF | |
| 同義語 | Isaglitazone,Netoglitazone,RWJ 241947 | ||
| Chemical Name | 5-[[6-[(2-fluorophenyl)methoxy]-2-naphthalenyl]methyl]-2,4-thiazolidinedione | ||
| Canonical SMILES | FC1=CC=CC=C1COC2=CC(C=CC(CC3SC(NC3=O)=O)=C4)=C4C=C2 | ||
| Formula | C21H16FNO3S | M.Wt | 381.4 |
| 溶解度 | ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| 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 | 2.6219 mL | 13.1096 mL | 26.2192 mL |
| 5 mM | 0.5244 mL | 2.6219 mL | 5.2438 mL |
| 10 mM | 0.2622 mL | 1.311 mL | 2.6219 mL |
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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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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