1、Product Data SheetRosiglitazoneCat. No.: HY-17386CAS No.: 122320-73-4分式: CHNOS分量: 357.43作靶點: PPAR; TRP Channel; Autophagy; Ferroptosis作通路: Cell Cycle/DNA Damage; Membrane Transporter/Ion Channel; NeuronalSignaling; Autophagy; Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、month溶解性數據體外實驗 DMSO : 110 mg/mL (307.75 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.7978 mL 13.9888 mL 27.9775 mL5 mM 0.5596 mL 2.7978 mL 5.5955 mL10 mM 0.2798 mL 1.3989 mL 2.7978 mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80

3、C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現現配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolub

4、ility: 2.75 mg/mL (7.69 mM); Clear solution此案可獲得 2.75 mg/mL (7.69 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (7.69 mM); Clear solutionPage 1 o

5、f 2 www.MedChemE此案可獲得 2.75 mg/mL (7.69 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.69 mM); Clear solution此案可獲得 2.75 mg/mL (7.69 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 27.5 mg/m

6、L 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Rosiglitazone (BRL 49653) ，100 nM 和 60 nM1。種選擇性的PPAR 激活劑，對 PPAR1，PPAR2 和 PPAR 的EC50 分別為 30 nMIC & Target PPAR1 PPAR2 TRPC5 TRPM230 nM (EC50) 100 nM (EC50)TRPM3體外研究 Rosiglitazone is a potent and selective activator of PPAR, with EC50s of 30 nM and

7、100 nM for PPAR1 and PPAR2,respectively, and a Kd of appr 40 nM for PPAR. Rosiglitazone (BRL49653, 0.1, 1,10 M) promotes differentiation ofC3H10T1/2 stem cells to adipocytes1. Rosiglitazone (Compound 6) activates PPAR, with an EC50 of 60 nM2.Rosiglitazone (1 M) activates PPAR, which binds to NF-1 pr

8、omoter to activate gene transcription in neurons.Rosiglitazone (1 M) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulatesBCL-2 expression in an NF-1-dependent manner3. Rosiglitazone completely inhibits TRPM3 with IC50 values of 9.5and 4.6 M against nifedipin

9、e- and PregS-evoked activity, but such effects are not via PPAR. Rosiglitazone inhibitsTRPM2 at higher concentration, with an IC50 of appr 22.5 M. Rosiglitazone is a strong stimulator of TRPC5 channels,with an EC50 of -30 M4.體內研究 Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic

10、rats. Rosiglitazone also decreases IL-6, TNF-,and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared todiabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by asignificantly lower contractile re

11、sponse to PE and Ang II and enhancement of ACh-provoked relaxation in aortasisolated from diabetic rats5.PROTOCOLKinase Assay 1 cDNA encoding amino acids 174-475 of PPAR1 is amplified via polymerase chain reaction and inserted intobacterial expression vector pGEX-2T. GST-PPAR LBD is expressed in BL2

12、1(DE3)plysS cells and extracts. For saturationbinding analysis, bacterial extracts (100 g of protein) are incubated at 4C for 3 h in buffer containing 10 mM Tris(pH 8.0), 50 mM KCl, 10 mM dithiothreitol with 3H-BRL49653 (specific activity, 40 Ci/mmol) in the presence orabsence of unlabeled Rosiglita

13、zone. Bound is separated from free radioactivity by elution through 1-mL Sephadex G-25 desalting columns. Bound radioactivity eluted in the column void volume and is quantitated by liquid scintillationcounting1.MCE has not independently confirmed the accuracy of these methods. They are for reference

14、 only.Cell Assay 1 C3H10T1/2 cells are grown in a 24-well plate in DME medium supplemented with 10% fetal calf serum. Medium and compound (Rosiglitazone) are exchanged every 3 days. Cells are stained at day 7 with Oil Red O and photographedPage 2 of 3 www.MedChemE1.MCE has not independently confirme

15、d the accuracy of these methods. They are for reference only.Animal Rats are intravenously injected with 38 mg/kg streptozotocin and after 48 h, diabetes is identified by urinaryAdministration 2 glucosuria and then random blood sugar is measured and this day is regarded as day 0. Animals with a seru

16、mglucose level of 220-300 mg/dL are selected to be used in this study. Rats are randomly separated into five groupsfor daily drug administration for 8 weeks: group 1: control nondiabetic rats given a vehicle only (0.5 mL/kg of 0.5%carboxy methyl celleluse orally), group 2: control diabetic rats give

17、n a vehicle, group 3: diabetic rats receivingRosiglitazone (5 mg/kg orally), group 4: diabetic rats receiving losartan (2 mg/kg, orally), and group 5: diabetic ratsreceiving both Rosiglitazone and losartan2.MCE has not independently confirmed the accuracy of these methods. They are for reference onl

18、y.戶使本產品發表的科研獻 Br J Pharmacol. 2020 Jan 23. Free Radic Biol Med. 2018 Aug 21;126:259-268. Pharmacol Res. 2020 Jan 31;153:104679. Am J Cancer Res. 2020 Apr 1;10(4):1182-1193. J Cell Mol Med. 2019 Aug 23.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Lehmann JM, et al.

19、 An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J BiolChem. 1995 Jun 2;270(22):12953-6.2. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemicactivity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8.3. Thouennon E, et al. Rosiglitazone-activated PPAR induce