Rosiglitazone - CAS 122320-73-4
Catalog number: 122320-73-4
Category: Inhibitor
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Molecular Formula:
C18H19N3O3S
Molecular Weight:
357.43
COA:
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Targets:
PPAR
Description:
Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively.
Purity:
>98%
Synonyms:
BRL 49653
MSDS:
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InChIKey:
YASAKCUCGLMORW-UHFFFAOYSA-N
InChI:
InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)
Canonical SMILES:
CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3
1.Novel Therapeutics for Diabetes: Uptake, Usage Trends, and Comparative Effectiveness.
Ahuja V1, Chou CH2. Curr Diab Rep. 2016 Jun;16(6):47. doi: 10.1007/s11892-016-0744-4.
The number of available therapies for treating type 2 diabetes has grown considerably in recent years. This growth has been fueled by availability of newer medications, whose benefits and risks have not been fully established. In this study, we review and synthesize the existing literature on the uptake, efficacy, safety, and cost-effectiveness of novel antidiabetic agents. Specifically, we focus on three drug classes that were introduced in the market recently: thiazolidinediones (TZDs), dipeptidyl peptidase-4 (DPP-4) inhibitors, and glucagon-like peptide-1 (GLP-1) receptor agonists. Not surprisingly, we find that the usage trends reflect the efficacy and safety profile of these novel drugs. The use of TZDs increased initially but decreased after a black-box warning was issued for rosiglitazone in 2007 that highlighted the cardiovascular risks associated with using the drug. Conversely, DPP-4 inhibitors and GLP-1 receptor agonists gained market shares due to their efficacy in glycemic control as an add-on treatment to metformin.
2.Minimally invasive surgery for ICH evacuation followed by rosiglitazone infusion therapy increased perihematomal PPARγ expression and improved neurological outcomes in rabbits.
Wu G1, Wu J1, Wang L1, Jiao Y1, Zhou H2, Tang Z3. Neurol Res. 2016 Apr 15:1-8. [Epub ahead of print]
OBJECTIVES: To observe the effects of minimally invasive surgery (MIS) for intracerebral hematoma (ICH) evacuation followed by rosiglitazone infusion therapy on peroxisome proliferator-activated receptor-gamma (PPARγ), blood-brain barrier (BBB) permeability, and neurological function.
3.Chronic stress and rosiglitazone increase indices of vascular stiffness in male rats.
Goodson ML1, Packard AE2, Buesing DR3, Maney M2, Myers B2, Fang Y1, Basford JE4, Hui DY4, Ulrich-Lai YM2, Herman JP2, Ryan KK5. Physiol Behav. 2016 Mar 31. pii: S0031-9384(16)30117-2. doi: 10.1016/j.physbeh.2016.03.031. [Epub ahead of print]
Prolonged and/or frequent exposure to psychological stress responses may lead to deterioration of organs and tissues, predisposing to disease. In agreement with this, chronic psychosocial stress is linked to greater cardiovascular risk, including increased incidence of atherosclerosis, myocardial ischemia, coronary heart disease, and death. Thus the association between stress and cardiovascular dysfunction represents an important node for therapeutic intervention in cardiovascular disease. Here we report that 2weeks of chronic variable stress (CVS) increased indices of vascular stiffness, including increased collagen deposition in the aortic adventitia and increased resting pulse pressure, in male rats. Thus CVS may represent a useful rodent model for stress-associated CVD, especially for aging populations for which widening pulse pressure is a well-known risk factor. Additionally, we report that the thiazolidinedione Rosiglitazone (RSG) blunts chronic stress-associated increases in circulating corticosterone.
4.Dipeptidyl peptidase-4 inhibitors and heart failure: Analysis of spontaneous reports submitted to the FDA Adverse Event Reporting System.
Raschi E1, Poluzzi E1, Koci A1, Antonazzo IC1, Marchesini G2, De Ponti F3. Nutr Metab Cardiovasc Dis. 2016 Feb 19. pii: S0939-4753(15)30192-7. doi: 10.1016/j.numecd.2016.02.006. [Epub ahead of print]
BACKGROUND AND AIMS: We tested the possible association between dipeptidyl peptidase-4 inhibitors (DPP-4-I) use and heart failure (HF) occurrence by assessing the publicly available US-FDA Adverse Event Reporting System (FAERS).
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CAS 122320-73-4 Rosiglitazone

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