Rosiglitazone
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| رقم الكتالوجGC16444 |
منشط PPARγ
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 122320-73-4
Sample solution is provided at 25 µL, 10mM.
Rosiglitazone is an orally active peroxisome proliferator-activated receptor gamma (PPARγ) selective agonist that selectively activates chimeras containing the PPARγ ligand-binding domain (LBD) but not PPARα and PPARδ with an EC50 of 60 nM and a Kd of 40nM[1, 2]. Rosiglitazone is an activator of transient receptor potential channel 5 (TRPC5) (EC50 of 30μM) and an inhibitor of transient receptor potential cation channel subfamily M member 3 (TRPM3) [3].
In vitro, treatment of hippocampal neurons with rosiglitazone (1 μM) for 24 or 48 h induced an increase in intracellular NF-α1 and BCL-2 protein levels [4]. Treatment of A2780 and SKOV3 cells with rosiglitazone (0-50 μM) for 7 days inhibited cell proliferation in a time-dependent and concentration-dependent manner [5].
In vivo, treatment of high-fat diet-fed obese mice with rosiglitazone (8 mg/kg) by intraperitoneal injection for 10 days reversed the abnormal molecular and cellular phenotypes of adipocytes [6]. Rosiglitazone (5 mg/kg) was orally administered to diabetic rats for 8 weeks and reduced the levels of IL-6, TNF-α, and VCAM-1, lipid peroxidation and nitric oxide, and increased aortic glutathionease and superoxide dismutase levels [7].
References:
[1] Bhagavathula N, Nerusu K C, Lal A, et al. Rosiglitazone inhibits proliferation, motility, and matrix metalloproteinase production in keratinocytes[J]. Journal of investigative dermatology, 2004, 122(1): 130-139.
[2] Lehmann J M, Moore L B, Smith-Oliver T A, et al. An antidiabetic Thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor(PPARγ)[J]. Journal of Biological Chemistry, 1995, 270(22): 12953-12956.
[3] Majeed Y, Bahnasi Y, Seymour V A L, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels[J]. Molecular pharmacology, 2011, 79(6): 1023-1030.
[4] Thouennon E, Cheng Y, Falahatian V, et al. Rosiglitazone‐activated PPAR γ induces neurotrophic factor‐α1 transcription contributing to neuroprotection[J]. Journal of neurochemistry, 2015, 134(3): 463-470.
[5] Wang Z, Gao J, Ohno Y, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib[J]. Cancer Chemotherapy and Pharmacology, 2020, 85: 273-284.
[6] Roh H C, Kumari M, Taleb S, et al. Adipocytes fail to maintain cellular identity during obesity due to reduced PPARγ activity and elevated TGFβ-SMAD signaling[J]. Molecular metabolism, 2020, 42: 101086.
[7] Ateyya H, Nader M A, El-Sherbeeny N A. Beneficial effects of rosiglitazone and losartan combination in diabetic rats[J]. Canadian Journal of Physiology and Pharmacology, 2018, 96(3): 215-220.
| Cell experiment [1]: | |
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Cell lines |
Neuron2A cells |
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Preparation Method |
Cells were treated with 1μM rosiglitazone for 24 or 48 h. |
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Reaction Conditions |
1μM; 24 or 48 h |
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Applications |
Rosiglitazone treatment increased the levels of intracellular NF-α1 and BCL-2 proteins. |
| Animal experiment [2]: | |
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Animal models |
Offspring of the hybrid between NuTRAP mice and Adipoq-Cre mice. |
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Preparation Method |
NuTRAP mice were crossed with Adipoq-Cre mice. The mice were placed on a chow diet or high-fat diet (HFD) at 6 weeks of age for 10 weeks. Rosiglitazone stock solution was prepared by dissolving in dimethyl sulfoxide (DMSO) at a concentration of 50 mg/ml. The stock solution was freshly diluted on each day prior to injection in saline containing 2% Tween 80 at a concentration of 1.6mg/ml of Rosiglitazone(3.2% of the stock) and IP injected into mice at a dose of 8 mg/kg for 10 consecutive days. |
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Dosage form |
8mg/kg; i.p. |
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Applications |
Rosiglitazone treatment reverses the molecular and cellular phenotypes in adipocytes associated with HFD. |
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References: [1] Thouennon E, Cheng Y, Falahatian V, et al. Rosiglitazone‐activated PPAR γ induces neurotrophic factor‐α1 transcription contributing to neuroprotection[J]. Journal of neurochemistry, 2015, 134(3): 463-470. [2] Roh H C, Kumari M, Taleb S, et al. Adipocytes fail to maintain cellular identity during obesity due to reduced PPARγ activity and elevated TGFβ-SMAD signaling[J]. Molecular metabolism, 2020, 42: 101086. |
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| Cas No. | 122320-73-4 | SDF | |
| المرادفات | BRL 49653 | ||
| Chemical Name | 5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3 | ||
| Formula | C18H19N3O3S | M.Wt | 357.43 |
| الذوبان | 100mg/ml in DMSO | Storage | Store at 2-8°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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7978 mL | 13.9888 mL | 27.9775 mL |
| 5 mM | 559.6 μL | 2.7978 mL | 5.5955 mL |
| 10 mM | 279.8 μL | 1.3989 mL | 2.7978 mL |
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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.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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