Cholic-acid - Endogenous Metabolite - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECholic acidCat. No.: HY-N0324CAS No.: 81-25-4分式: CHO分量: 408.57作靶點(diǎn): Endogenous Metabolite作通路: Metabolic Enzyme/Protease儲(chǔ)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(shí)驗(yàn) DMSO : 50 mg/mL (122.38 mM)H2O

2、 : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.12 mM); Clear solution2. 請(qǐng)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 solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.12 mM); Clea

3、r solutionBIOLOGICAL ACTIVITY物活性 Cholic acid肝臟中產(chǎn)的主 膽汁酸，通常與氨酸或磺酸綴合，有助于脂肪吸收和膽固醇排泄。IC50 & Target Human Endogenous Metabolite體外研究 Cholic acid competitively binds Na+/taurocholate cotransporting polypeptide (NTCP) on HepG2 cells andsignificantly inhibits the uptake of Cholic acid (CA)-nanoliposomes (LPs)

4、-Doxorubicin (DOX)-HCl, whichindicates that CA-LPs-DOX-HCl are also uptaken via NTCP-mediated endocytosis pathway 1.體內(nèi)研究 Cholic acid feeding leads to increased CYP2D6 expression in CYP2D6-humanized mice. As a cholestasismodel, Tg-CYP2D6 mice are fed a Cholic acid (CA)-supplemented diet for over 1 we

5、ek. The treatment isknown to increase bile acid pool size by 2-fold and to replace 90% of bile acids with CA, recapitulating thefeatures of cholestatic conditions in humans 2.PROTOCOLCell Assay 1 HepG2 cells are pretreated with the inhibitors NaN3 (1 mg/mL), Genistein (50 g/mL), MCD (10 mM),Nystatin

6、 (50 g/mL), Chlorpromazine (10 g/mL), and Cholic acid (1 mg/mL) for 30 min. After removing theinhibitors, the cells are incubated with CA-LPs for 2 h, and the cellular uptake of LPs is determined in the Invitro cellular uptake assays section 1.MCE has not independently confirmed the accuracy of thes

7、e methods. They are for reference only.Animal Mice 2Administration 2 Tg-CYP2D6 mice are fed with normal chow (control) or 1% (w/w) Cholic acid-supplemented diet (CA) for 14days (n=4 mice/group). Alkaline phosphatase (ALP) and alanine aminotransferase (ALT) activities aremeasured in mouse serum.MCE h

8、as not independently confirmed the accuracy of these methods. They are for reference only.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Res. 2019 Mar;29(3):193-205.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Li Y, et al. Mechanism of hepatic targeting via oral administration of DSPE-PEG-Cholic acid-mod

9、ified nanoliposomes. Int JNanomedicine. 2017 Feb 28;12:1673-1684.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. Pan X, et al. Cholic acid Feeding Leads to Increased CYP2D6 Expression in CYP2D6-Humanized Mice. Drug Metab Dispos. 2017Apr;45(4):346-352.McePdfHeightCaution: Product has not been fully validated for medical