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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETroxerutinCat. No.: HY-N0139CAS No.: 7085-55-4Synonyms: Trihydroxyethylrutin分式: CHO分量: 742.68作靶点: NOD-like Receptor (NLR)作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验

2、 DMSO : 100 mg/mL (134.65 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.3465 mL 6.7324 mL 13.4647 mL5 mM 0.2693 mL 1.3465 mL 2.6930 mL10 mM 0.1346 mL 0.6732 mL 1.3465 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Troxerutin 也被称为维素 P4,天然物类

3、 酮芦丁的三羟 化衍物,其可抑制活性氧 (ROS) 的产并抑制 ER 应激介导的 NOD 活化。IC50 & Target ROS 1, NOD 2体外研究The results reveal that the maximum protective effect against ROS induced cell damage in the HDP cells1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEoccurs following pretreatment with 10 M Troxerutin. Treatment with H2O2

4、 alone decreases cell viability to77.332.44%; however, pretreatment with 10 M Troxerutin maintains cell viability at 90.882.24% followingH2O2 exposure (P2O2 alone increases the level of ROS to 46.362.33%. The cells pretreated withTroxerutin are 19.921.95% DCF-positive following H2O2 treatment, indic

5、ating that Troxerutin reduces theH2O2-induced production of ROS in the HDP cells 1 .体内研究 Troxerutin effectively lowers body weight and obesity-related metabolic parameters in high-fat diet (HFD)-treated mice. Oral administration of Troxerutin notably inhibits those liver injuries in HFD-treated mice

6、,restores glucose intolerance and insulin signaling, and diminishes hepatic gluconeogenesis in HFD-treatedmice. Troxerutin remarkably inhibits the nuclear translocation of NF-B p65, as well as the expressions of itstarget genes, in the livers of HFD-treated mice. Troxerutin also depresses endoplasmi

7、c reticulum (ER)stress-mediated Nucleotide oligomerization domain (NOD) activation in HFD-treated mouse livers 2. Lipiddepositions in tunica intimae and tunica media are attenuated in Troxerutin-treated diabetic rats comparewith untreated diabetic rats. Structural disarrangement and deformity of smo

8、oth muscle cells in aortic tissueof Troxerutin-treated diabetic rats are considerably lower than histology of untreated diabetic aorta.Administration of Troxerutin for four weeks to diabetic rats significantly reduces the level of malondialdehyde(MDA) compare to that of untreated diabetic rats (P 3.

9、PROTOCOLCell Assay 1 The cells are plated at a density of 4103/well in a 96-well plate. At 70 to 80% confluence, the cells aretreated with Troxerutin at concentrations ranging between 0 and 60 M for 24 h at 37C. Subsequently, 10 L water soluble tetrazolium salt assay solution is added to each well a

10、nd, following incubation for 30 min at37C, the optical density is measured at 490 nm using a reader. To examine Troxerutin mediated ROSprotection, the cells are pretreated with Troxerutin at the following concentrations: 0, 5, 10 and 15 M for 8 h.Subsequently, 750 M H2O2 is added to each well. Follo

11、wing incubation for 24 h at 37C, cell viability isevaluated using an Cell Viability Assay kit. The level of cell viability (%) is normalized to that of 0.1%dimethyl-sulfoxide (DMSO)-treated cells. Each experiment is repeated at least three times 1.MCE has not independently confirmed the accuracy of

12、these methods. They are for reference only.Animal Thirty two adult male Wistar rats weighing 250 to 300 grams are used in this study. The animals areAdministration 3 randomly divided into four groups (n=8/each) as: group I: control (C), group II: control with Troxerutin(C+TXR), group III: diabetic (

13、D), and group IV: diabetic with Troxerutin (D+TXR). The control rats arereceived the same amount of citrate buffer alone. Development of diabetes is confirmed by measuring bloodglucose levels, 72 hours later. Animals with blood glucose levels higher than 16.65 mM (300 mg/dL) areconsidered diabetic a

14、nd those with blood glucose levels lower than this value are excluded from theexperiment. Troxerutin (150 mg/kg/day) is administered orally, once daily for four weeks. After 10 weeks ofinduction of diabetes, diabetic animals as well as the time-matched controls are killed and aortic samples arecolle

15、cted 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Lim KM, et al. Analysis of changes in microRNA expression profiles in response to the troxerutin-mediated antioxidant effect in humander

16、mal papilla cells. Mol Med Rep. 2015 Aug;12(2):2650-60.2. Zhang Z, et al. Troxerutin Attenuates Enhancement of Hepatic Gluconeogenesis by Inhibiting NOD Activation-Mediated Inflammation inHigh-Fat Diet-Treated Mice. Int J Mol Sci. 2016 Dec 25;18(1). pii: E31.3. Badalzadeh R, et al. Beneficial effect of troxerutin on diabetes-induced vascular damages in rat aorta: histopathological alterations andantioxidation mechanism. In

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