Tauroursodeoxycholate-TUDCA-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETauroursodeoxycholateCat. No.: HY-19696CAS No.: 14605-22-2Synonyms: TUDCA; UR 906; Taurolite分式: CHNOS分量: 499.7作靶點(diǎn): ERK; Caspase; Endogenous Metabolite; Apoptosis作通路: MAPK/ERK Pathway; Stem Cell/Wnt; Apoptosis; MetabolicEnzyme/Pr

2、otease儲(chǔ)存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Tauroursodeoxycholate (TUDCA; UR 906; Taurolite)種內(nèi)質(zhì)應(yīng)激抑制劑。Tauroursodeoxycholate 顯著降低凋亡分如 caspase-3 和 caspase-12 表達(dá)。Tauroursodeoxycholate 也抑制 ERK。IC50 & Target ERK Caspase-3 Caspase-12 Human Endogenou

3、sMetabolite體外研究 Tauroursodeoxycholate (TUDCA) suppresses both viability and migration of vascular smooth muscle cells(VSMCs) through inhibition of ERK phosphorylation, by induction of mitogen-activated protein kinasephosphatase-1 (MKP-1) via PKC. Tauroursodeoxycholate inhibits both the proliferation

4、 and migration ofVSMCs via inhibition of ERK, through Ca2+-dependent PKC translocation. Tauroursodeoxycholate preventsplatelet-derived growth factor (PDGF) and vascular injury-induced MMP-9 expression. The knock-down ofMKP-1 using specific si-RNA restores the reduced VSMC viability by Tauroursodeoxy

5、cholate (200 M),which suggests that anti-proliferative effect of Tauroursodeoxycholate depended on the MKP-1 expression1.體內(nèi)研究The effects of Tauroursodeoxycholate (TUDCA) on proliferation and apoptosis of VSMCs in vivo areexamined using immunohistochemistry for proliferating cell nuclear antigen (PCN

6、A) and the transferasedUTP nick-end labelling (TUNEL) assay. Tauroursodeoxycholate (10, 50, and 100 mg/kg) increases thecaspase 3 activity of injured tissues in a dose-dependent manner, indicating that Tauroursodeoxycholateinduces apoptosis of VSMCs in the neointima. Using the injured tissues, furth

7、er examination and comparisonof the phosphorylation level of ERK and MMP-9 expression is performed at 1 week after injury, compared1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEwith normal controls. Balloon injury increased both the phosphorylation of ERK and expression of MMP-9 inthe tissues. Ta

8、uroursodeoxycholate (10, 50, and 100 mg/kg) inhibits phosphorylation of ERK and MMP-9expression in a dose-dependent manner 1. Tauroursodeoxycholate (TUDCA) is a hydrophilic bile acid.Tauroursodeoxycholate as a cytoprotective agent improves liver function and can prevent hepatocellularcarcinoma by re

9、ducing ER stress and apoptosis. Tauroursodeoxycholate significantly reduces expression ofapoptosis molecules, such as caspase-3, caspase-12, C/EBP homologous protein, c-Jun N-terminal kinase(JNK), activating transcription factor 4 (ATF4), X-box binding protein (XBP), and eukaryotic initiation factor

10、 2(eIF2) in Ang II induced ApoE-/- mice (p-/- mice. Tauroursodeoxycholate is used at a dose of 0.5 g/kg/day intreating Ang II induced ApoE-/- mice (ER stress inhibitor group). Systolic blood pressure (141.35.6 mmHgvs 145.98.9 mmHg; p0.05) and total cholesterol levels (663.688.7 mg/dL vs 655.765.4 mg

11、/dL; p0 .05)do not differ between the AAA model group and Tauroursodeoxycholate group. In addition, maximum aorticdiameter is significantly smaller in those in Tauroursodeoxycholate group compared with those in the AAAmodel group (0.950.03 mm vs 1.790.04 mm; p2 vs 1.510.06 mm2; p 2.PROTOCOLCell Assa

12、y 1 Cell viability and proliferation are measured using Ez-Cytox. VSMCs (5103 cells) are seeded onto 96-wellplates in Smooth Muscle Cell Growth Medium 2 (SMCGM2) and cultured. After serum starvation,Tauroursodeoxycholate (0, 50, 100, and 200 M) is added to the hVSMCs, with or without 1,2-bis(o-amino

13、phenoxy) ethane-N,N,N,N-tetraacetic acid tetra(acetoxymethyl) ester (BAPTA, 10 M) and 7-hydroxystaurosporine (H7, 10 M) and cultured for 24 h. To assess the effect of Tauroursodeoxycholate onthe PDGF-stimulated hVSMC proliferation, hVSMCs are seeded onto 96-well plates and cultured. Afterserum starv

14、ation, Tauroursodeoxycholate (0, 50, 100, and 200 M) is added to the hVSMCs, with or withoutPDGF-BB (50 ng/mL) and cultured. After addition of 10 L of Ez-Cytox into each well, cell viability isevaluated by measuring the optical density at 450 nm 1.MCE has not independently confirmed the accuracy of

15、these methods. They are for reference only.Animal Rats 1Administration 12 Sprague-Dawley rats are anaesthetized with a combined anaesthetic (Ketamine, 70 mg/kg; Xylazine, 7mg/kg ip). Tauroursodeoxycholate is administered orally once a day, in different concentrations (i.e. vehicle,10, 50, and 100 mg

16、/kg) for 2 weeks. The carotid arteries are fixed by perfusion with 4% formaldehyde, thenthe tissues are embedded in paraffin, and sections (8 m) are stained with H&E 1.Mice 2Thirty ApoE-/- C57BL/6 male mice aged 8 weeks are randomly divided into three groups (n=10 in eachgroup): (i) sham operated an

17、d injected with physiologic (0.9%) saline as vehicle (normal: group); (ii) mini-osmotic pumps are implanted subcutaneously into the right flank of ApoE-/- mice to release Ang II (1000ng/kg/min) over the course of 28 days (AAA model group); (iii) AAA model mice treated withTauroursodeoxycholate daily

18、 for 4 weeks at a dosage of 0.5 g/kg/day in drinking water(Tauroursodeoxycholate group). Mice are sacrificed after 28 days of Ang II infusion 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Br J Pharmacol. 2019 Jul;176(13):2162-2178. Biochem Pharmacol. 2018 May 24;154:278-292. J Cell Mol Med. 2019 Aug 23. Sci Rep. 2017 Aug 30;7(1):9967. Food Chem Toxicol. 2018 Jul 14;120:253-260.See more customer validations on HYPERLINK / www.MedChemEREFERENCES