膽酸作用機制 - Medchemexpress - MCE中國

1、Product Data SheetCholic acidCat. No.: HY-N0324CAS No.: 81-25-4分式: CHO分量: 408.57作靶點: Endogenous Metabolite作通路: Metabolic Enzyme/Protease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 DMSO : 50 mg/mL (122.38 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturatio

2、n unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.4476 mL 12.2378 mL 24.4756 mL5 mM 0.4895 mL 2.4476 mL 4.8951 mL10 mM 0.2448 mL 1.2238 mL 2.4476 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；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實

3、驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?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(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)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(xiàn)沉淀、析出現(xiàn)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% salineSolubility: 2.5 mg/mL (6.12 mM); Clear solution此案可獲得 2.5 mg/mL (6.12 mM，飽和度未知)

4、 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 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(xù)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: 2.5 mg/mL (6.12 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (6.12 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25

5、.0 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: 2.5 mg/mL (6.12 mM); Clear solution此案可獲得 2.5 mg/mL (6.12 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 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Cholic acid肝臟中產(chǎn)的主 膽汁酸，通常與氨

6、酸或磺酸綴合，有助于脂肪吸收和膽固醇排泄。IC & Target Human Endogenous Metabolite體外研究 Cholic acid competitively binds Na+/taurocholate cotransporting polypeptide (NTCP) on HepG2 cells and significantlyinhibits the uptake of Cholic acid (CA)-nanoliposomes (LPs)-Doxorubicin (DOX)-HCl, which indicates that CA-LPs-DOX-HCl a

7、re also uptaken via NTCP-mediated endocytosis pathway1.體內(nèi)研究 Cholic acid feeding leads to increased CYP2D6 expression in CYP2D6-humanized mice. As a cholestasis model, Tg-CYP2D6 mice are fed a Cholic acid (CA)-supplemented diet for over 1 week. The treatment is known to increase bileacid pool size by

8、 2-fold and to replace 90% of bile acids with CA, recapitulating the features of cholestaticconditions in humans2.PROTOCOLCell Assay 1 HepG2 cells are pretreated with the inhibitors NaN3 (1 mg/mL), Genistein (50 g/mL), MCD (10 mM), Nystatin (50 g/mL), Chlorpromazine (10 g/mL), and Cholic acid (1 mg/

9、mL) for 30 min. After removing the inhibitors, the cells areincubated with CA-LPs for 2 h, and the cellular uptake of LPs is determined in the In vitro cellular uptake assayssection1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administra

10、tion 2 Tg-CYP2D6 mice are fed with normal chow (control) or 1% (w/w) Cholic acid-supplemented diet (CA) for 14 days(n=4 mice/group). Alkaline phosphatase (ALP) and alanine aminotransferase (ALT) activities are measured in mouseserum.MCE has not independently confirmed the accuracy of these methods.

11、They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Cell Res. 2019 Mar;29(3):193-205.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCESPage 2 of 3 www.MedChemE1. Li Y, et al. Mechanism of hepatic targeting via oral administration of DSPE-PEG-Cholic acid-modified nanoliposomes. Int J Nanomedicine. 2017 Feb28;12:1673-1684.2. Pan X, et al. Cholic acid Feeding Leads to Increased CYP2D6 Expression in CYP2D6-Humanized Mice. Drug Metab Dispos. 2017 Apr;45(4):346-352.McePdfHeightCaution: Product has not been fully