Inolitazone - CAS 223132-37-4
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Not Intended for Therapeutic Use. For research use only.
Inolitazone is an orally bioavailable PAPR-gamma inhibitor with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction of tumor cell differentiation and apoptosis, and so a reduction in tumor cell proliferation. PPAR-gamma is a nuclear hormone receptor and ligand-activated transcription factor controlling gene expression involved in such cellular processes as differentiation, apoptosis, cell-cycle control, carcinogenesis, and inflammation.
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PPAR-gamma agonist CS-7017, CS-7017, RS5444. Efatutazone.
Current Developer:
Daiichi Sankyo.
1.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.
2.Glucose-lowering therapy in type 2 diabetes : New hope after the EMPA-REG outcome trial.
Schernthaner G1, Schernthaner GH2. Herz. 2016 Apr 12. [Epub ahead of print]
Prevention of cardiovascular morbidity and mortality remains the key factor in the treatment of type 2 diabetes (T2DM). In the early phase of T2DM, multifactorial intervention is mandatory and glucose levels should be near normal, in particular in younger patients presenting with the highest cardiovascular risk. Anti-diabetic drugs without any risk for hypoglycaemia should be preferred in order to reduce clinical inertia and increase the long-term adherence to the treatment. In patients already presenting with cardiovascular disease, the best outcome may be expected with the triple oral therapy of metformin, pioglitazone, and empagliflozin, although a controlled prospective study versus insulin therapy is needed to confirm the expectation.
3.Characterizing the Dissolution Profiles of Supersaturable Salts, Cocrystals, and Solvates to Enhance In Vivo Oral Absorption.
Hisada N1, Takano R1, Takata N1, Shiraki K1, Ueto T1, Tanida S1, Kataoka M2, Yamashita S3. Eur J Pharm Biopharm. 2016 Apr 6. pii: S0939-6411(16)30128-X. doi: 10.1016/j.ejpb.2016.04.004. [Epub ahead of print]
The purposes of this study were to elucidate the type-specific characteristics of salt, cocrystal, and solvate formulations upon dissolution and precipitation, and to clarify their effect on enhancing oral absorption. Several types of solid formulations (dantrolene sodium salt [DAN-NA], pioglitazone hydrochloride salt [PIO-HCL], megestrol acetate saccharin cocrystal [MEG-SA], and an in-house compound ZR ethanolate [ZR-ETH]) that induce supersaturation of BCS class II drugs were compared to their crystalline free forms. An in vitro miniscale dissolution test in biorelevant media was used to characterize their dissolution profiles and residue forms. Both salts (DAN-NA and PIO-HCL) rapidly reached the maximum concentration within 5 minutes, whereas the cocrystal (MEG-SA) did so slowly. After the maximum concentration had been reached, the dissolved concentrations of DAN-NA, PIO-HCL, and MEG-SA decreased, but that of ZR-ETH did not. Time-dependent XRPD analysis revealed that the initial solid state of each salt dissolved within 5 minutes, whereas the cocrystal remained for more than 10 minutes, and the solvate remained for 4 hours.
4.Identification and modification of amyloid-independent phenotypes of APOE4 mice.
DiBattista AM1, Dumanis SB1, Newman J1, Rebeck GW2. Exp Neurol. 2016 Apr 13. pii: S0014-4886(16)30094-2. doi: 10.1016/j.expneurol.2016.04.014. [Epub ahead of print]
BACKGROUND: Over 70 million Americans inherit the strongest genetic risk factor for Alzheimer's disease (AD), apolipoprotein E4 (APOE4), but have no course for reducing their risk. The association of non-steroidal anti-inflammatory drug (NSAID) use with reduced risk of AD for APOE4-carriers suggests that NSAIDs may be useful in AD prevention.
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CAS 223132-37-4 Inolitazone

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