Pioglitazone - CAS 111025-46-8
Catalog number: 111025-46-8
Category: Inhibitor
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Molecular Formula:
C19H20N2O3S
Molecular Weight:
356.44
COA:
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Targets:
PPAR
Description:
Pioglitazone significantly attenuates left ventricular (LV) cavity dilatation and dysfunction by echocardiography as well as LV end-diastolic pressure in mice with extensive anterior myocardial infarction.
Purity:
>98%
Synonyms:
N/A
MSDS:
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InChIKey:
HYAFETHFCAUJAY-UHFFFAOYSA-N
InChI:
InChI=1S/C19H20N2O3S/c1-2-13-3-6-15(20-12-13)9-10-24-16-7-4-14(5-8-16)11-17-18(22)21-19(23)25-17/h3-8,12,17H,2,9-11H2,1H3,(H,21,22,23)
Canonical SMILES:
CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
1.Generalized intense pruritus during canagliflozin treatment: Is it an adverse drug reaction?
Vasapollo P, Cione E, Luciani F, Gallelli L1. Curr Drug Saf. 2016 Apr 5. [Epub ahead of print]
Selective agents able to locate and identify unique targets represent a crucial aspect of modern pharmacology. The exclusive location of sodium-glucose co-transporter-2 (SGLUT2) on kidneys prompt companies to develop SGLT2 inhibitors that today are the latest class of drugs for diabetes treatment. In particular, canagliflozin blocks the re-absorption of glucose in the kidney lowering blood glucose levels by increasing glucose excretion. We report a 61-year old woman who developed an intense and severe pruritus during the treatment with canagliflozin. Clinical and laboratory findings excluded the presence of systemic or skin diseases able to induce pruritus. The discontinuation of canagliflozin and the treatment with pioglitazone/metformin fixed combination induced a remission of pruritus. This case emphasizes the need to consider pruritus as a differential diagnosis during the treatment with canagliflozin.
2.Pioglitazone alleviates inflammation in diabetic mice fed a high-fat diet via inhibiting advanced glycation end product (AGE)-induced classical macrophage activation.
Jin X1,2, Liu L2, Zhou Z1,2, Ge J3, Yao T4, Shen C2. FEBS J. 2016 Apr 8. doi: 10.1111/febs.13735. [Epub ahead of print]
Classically activated macrophages (M1) are associated with inflammation in diabetic patients. Inflammation is a known risk factor in diabetes. This study tested the hypothesis that pioglitazone (PIO) alleviates inflammation in diabetic mice fed a high-fat diet by inhibiting advanced glycation end product (AGE)-induced classical macrophage activation. Indeed, we found that AGE treatment promoted transcription of pro-inflammatory molecules and M1 surface markers, but that PIO increased the expression of anti-inflammatory genes and decreased the expression of pro-inflammatory mediators in bone marrow derived macrophages (BMDMs) in a dose-dependent manner. Furthermore, pretreatment with PIO abrogated the effects of AGE on pro-inflammatory markers and partly inhibited AGE-induced NFκB activation. PIO treatment partly reduced the inflammatory phenotype in diabetic ApoE-/- mice, and significantly reduced NFκB activation in plaques. Therefore, we conclude that pioglitazone blocks classical activation of macrophages and attenuates inflammation in mouse models of diabetes.
3.EASL-EASD-EASO Clinical Practice Guidelines for the management of non-alcoholic fatty liver disease: is universal screening appropriate?
Byrne CD1,2, Targher G3. Diabetologia. 2016 Apr 7. [Epub ahead of print]
Non-alcoholic fatty liver disease (NAFLD) is very common in people with type 2 diabetes and although estimates for the prevalence NAFLD vary according to age, obesity and ethnicity, some studies have indicated that up to 75% of patients with type 2 diabetes may be affected. During the last 15 years there has been a vast amount of research into understanding the natural history, aetiology and pathogenesis of NAFLD; and now there is a better understanding of the strengths and limitations of diagnostic tests for NAFLD, the influence of lifestyle changes and the effects of potential treatments. With this advance in knowledge, it is apposite that a number of organisations have started to develop guidelines for the diagnosis and management of NAFLD. Given the high proportion of patients with type 2 diabetes who are affected by this liver condition, it is now important to consider how any guideline will affect the care, diagnosis and treatment of patients with type 2 diabetes.
4.Suppression of connective tissue growth factor mediates the renoprotective effect of Sitagliptin rather than Pioglitazone in type 2 diabetes mellitus.
Ali SM1, Khalifa H2, Mostafa DK3, El Sharkawy A1. Life Sci. 2016 Apr 3. pii: S0024-3205(16)30192-8. doi: 10.1016/j.lfs.2016.03.043. [Epub ahead of print]
AIM: Diabetic nephropathy (DN) is a leading cause of end-stage renal disease, and thus, the ability of antidiabetic drugs to ameliorate renal microvascular disease may be as important as their ability to control blood glucose. Therefore, we investigated the reno-protective effect of the antidiabetic drugs, Sitagliptin and Pioglitazone, versus combined Metformin/Enalapril in a rat model of type 2 diabetes.
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CAS 111025-46-8 Pioglitazone

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