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化学情報
| Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C24H40O3 |
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| 分子量 | 376.57 | CAS No. | 434-13-9 | ||||
| Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (199.16 mM) | ||||
| Ethanol | 47 mg/mL (124.81 mM) | ||||||
| Water | Insoluble | ||||||
| 体内 （毎回新しく調製した物を用意してください） |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Lithocholic acidは、毒性のある二次胆汁酸であり、肝内胆汁うっ滞を引き起こし、腫瘍促進活性を持ちます。その毒性効果は、vitamin D receptor、PXR、FXRを活性化することで保護されます。 |
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| in vitro | Lithocholic acid (LCA) is a hydrophobic secondary bile acid that is primarily formed in the intestine by the bacterial 7α-dehydroxylation of chenodeoxycholic acid. LCA causes intrahepatic cholestasis (cessation or impairment of bile flow). LCA activates PXR (pregnane X receptor), and the LCA-induced severe liver damage can be protected by the activation of PXR. LCA can activate farnesoid X receptor (FXR) with EC50 of 3.8 μM. LCA directly binds VDR (vitamin D receptor) with Ki of 29μM, activates VDR (vitamin D receptor) 30 μM, with much more sensitivity than the other nuclear receptors (eg. PXR, FXR), and its toxic effect is thus protected. LCA has tumor-promoting activity, inhibits mammalian DNA Polymerase β with IC50 of 15 μM. |
| in vivo | Administration of LCA and its conjugates to rodents causes intrahepatic cholestasis,a pathogenic state characterized by decreased bile flow and the accumulation of bile constituents in the liver and blood. In DMH (dimethyldydrazine)-induced murine carcinogenesis model, LCA suppresses apoptosis almost completely in premalignant colon. LCA activates VDR, induces expression in vivo of CYP3A, a cytochrome P450 enzyme that detoxifies LCA in the liver and intestine. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Competitive ligand binding assay. | |
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| Ligand binding is performed using lysates from COS-7 cells transfected with expression plasmids for VDR or RXRα. Binding is performed overnight at 4°C in lysate buffer with 0.71 nM (18 Ci/mmol) [3H]1,25(OH)2D3 and bile acid competitor. Unbound [3H]1,25(OH)2D3 is removed by adsorption to dextran-coated charcoal and the supernatant removed for scintillation counting. Ki values are calculated from a computer fit of competition curves from triplicate assays. | ||
| 細胞アッセイ | 細胞株 | HEK293 |
| 濃度 | ~30 μM | |
| 反応時間 | ||
| 実験の流れ | Receptor specific activation by LCA. Various nuclear receptors are expressed in HEK293 cells and screened for activation by 30 μM LCA with a mammalian two-hybrid GAL4-SRC-1 and VP16-receptor luciferase assay. |
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| 動物実験 | 動物モデル | Mouse |
| 投薬量 | 0.125 mg/g, twice a day for 4 days. | |
| 投与方法 | i.p. | |
参考
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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Vitamin D3 suppresses the cholesterol homeostasis pathway in patient-derived glioma cell lines [ FEBS Open Bio, 2023, 13(9):1789-1806] | PubMed: 37489660 |
| Jiangzhi granule attenuates non-alcoholic steatohepatitis through modulating bile acid in mice fed high-fat vitamin D deficiency diet [ Biomed Pharmacother, 2022, 149:112825] | PubMed: 35305348 |
| Drug repositioning as a therapeutic strategy for neurodegenerations associated with OPA1 mutations [ Hum Mol Genet, 2020, ddaa244] | PubMed: 33231680 |
| Production of Functional Hepatobiliary Organoids from Human Pluripotent Stem Cells [ Int J Stem Cells, 2020, 10.15283/ijsc20152] | PubMed: 33377458 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。