胆酸作用机制 - Medchemexpress - MCE中国

1、Product Data SheetCholic acidCat. No.: HY-N0324CAS No.: 81-25-4分式: CHO分量: 408.57作靶点: Endogenous Metabolite作通路: Metabolic Enzyme/Protease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 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制备储备液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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实

3、验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.12 mM); Clear solution此案可获得 2.5 mg/mL (6.12 mM，饱和度未知)

4、 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.12 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (6.12 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25

5、.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.12 mM); Clear solution此案可获得 2.5 mg/mL (6.12 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Cholic acid肝脏中产的主 胆汁酸，通常与氨

6、酸或磺酸缀合，有助于脂肪吸收和胆固醇排泄。IC & Target Human Endogenous Metabolite体外研究 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.体内研究 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.户使本产品发表的科研献 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