Pioglitazone-hydrochloride-U-72107A-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPioglitazone hydrochlorideCat. No.: HY-14601CAS No.: 112529-15-4Synonyms: U 72107A; AD 4833分式: CHClNOS分量: 392.9作靶點: PPAR作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DM

2、SO : 100 mg/mL (254.52 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5452 mL 12.7259 mL 25.4518 mL5 mM 0.5090 mL 2.5452 mL 5.0904 mL10 mM 0.2545 mL 1.2726 mL 2.5452 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體

3、內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.36 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.36 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1

4、/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.36 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pioglitazone種有效，選擇性的 PPAR 激動劑，親和結(jié)合到 PPAR 配體結(jié)合域。作于和PPAR，EC50 分別為 0.93 和 0.99 M。IC50 & Target PPAR PPAR PPAR0.01 M (EC50, Human PPAR) 0.93 M (EC50, Human PPAR 43 M (EC50, Human PPAR)體外

5、研究 AGEs-induced beta cell necrosis is completely abrogated by adding Pioglitazone to the AGEs culturemedium. Furthermore Pioglitazone completely prevented any AGEs-induced increment in caspase-3activation, thereby restoring caspase-3 activity to the same levels as the control cells. As expected AG i

6、sable to counteract AGEs-induced impaired viability 2.體內(nèi)研究 The serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo-/- ob/ob miceare unchanged after 10 mg/kg Pioglitazone but are significantly reduced to a similar degree after 30 mg/kgPioglitazone. Moreover, th

7、e expressions of TNF and resistin in adipose tissues of ob/ob and adipo-/- ob/obmice are unchanged after 10 mg/kg Pioglitazone but are decreased after 30 mg/kg Pioglitazone. Thus,Pioglitazone-induced amelioration of insulin resistance and diabetes may occur adiponectin dependently inthe liver and ad

8、iponectin independently in skeletal muscle 3. Pioglitazone (10 mg/kg per d) treatmentsignificantly attenuates the loss of body weight (BW) and cardiac hypertrophy. Pioglitazone treatmentsignificantly reduces the elevated serum glucose levels and markedly improved the associated dyslipidemia.Furtherm

9、ore, there is a slight but significant increase in serum creatinine level in D rats over their N controls(P 4.PROTOCOLCell Assay 2 In order to evaluate cell proliferation, HIT-T15 cells are seeded on 96-well plates (3104 cells/well) andcultured for 5 days as described. Viable cells are determined us

10、ing the Cell Titer 96 Aqueous One SolutionCell Proliferation Assay. To evaluate cell apoptosis and cell necrosis, HIT-T15 cells are plated on 6-welldishes (7105 cells/well) for 5 days in standard conditions (CTR) or in the presence of AGEs (AGEs) with orwithout Pioglitazone (0.5 or 1 M) or AG (1 mM)

11、. They are then processed to measure both the activity ofcaspase-3 and the activity of lactate dehydrogenase (LDH) (a stable cytosolic enzyme that is a marker of cellmembrane damage and cell death due to necrosis) using Cytotox 96 Non Radioactive Cytotoxicity Assay 2.MCE has not independently confir

12、med the accuracy of these methods. They are for reference only.Animal Mice 3Administration 34 10 mg/kg Pioglitazone HCl or vehicle (0.25% carboxymethylcellulose) is adnimistered to ob/ob and adipo-/-ob/ob mice by oral gavage once daily for 14 consecutive days. 30 mg/kg Pioglitazone or vehicle is als

13、oadnimistered to ob/ob and adipo-/- ob/ob mice by oral gavage once daily for 14 consecutive days.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemERats 4Male Wistar albino rats (weighing 25020 g) are ued.Rats that achieved serum glucose level 250 mg/dLand serum creatinine level 1.5 mg/dL are divided

14、into 2 groups (n=10 per each group): diabeticnephropathic (DN) group in which rats received an equal amount of vehicle (0.5% carboxy methyl cellulose)and Pioglitazone-treated (DN+Pio) group in which rats treated with Pioglitazone. Pioglitazone (10 mg/kg BW)is given orally by gastric gavage, once dai

15、ly, for 4 weeks.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Nutr Metab. 2019 Mar. Int J Oncol. 2018 Aug;53(2):551-566. Am J Physiol Renal Physiol. 2019 Jul 1;317(1):F137-F151. J Diabetes Res. 2019 Feb 3;2019:5245063. Mol Med Rep. 2019 Ja

16、n;19(1):400-406.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Kuwabara K, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-4-5-methyl-2-(4-methylphenyl)-4-oxazolylbutyl-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases

17、 plasma triglyceride and glucose leve2. Puddu A, et al. Pioglitazone attenuates the detrimental effects of advanced glycation end-products in the pancreatic beta cell line HIT-T15. Regul Pept. 2012 Aug 20;177(1-3):79-84.3. Kubota N, et al. Pioglitazone ameliorates insulin resistance and diabetes by both adiponectin-dependent and -independent pathways. JBiol Chem. 2006 Mar 31;281(13):8748-55.4. Elrashidy RA, et al. Pioglitazone attenuates cardiac fibrosis and hypertrophy in a rat model of diabet