中文名稱:鵝去氧膽酸 | 英文名稱:Chenodeoxycholic acid |
CAS:474-25-9 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.97% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T0847 |
名稱 | Chenodeoxycholic acid |
描述 | Chenodeoxycholic acid (CDCA) is a bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones. |
細(xì)胞實(shí)驗(yàn) | The cell viability is analyzed by incubating transfected HEK-293 cells and CHO cells for 1 h with the corresponding concentration of bile acid and staining with trypan blue. The toxicity of bile acids is analyzed using the tetrazolium salt MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) according to the cell proliferation kit I. No significant differences between control and bile acid-treated cells are obtained in both tests. |
激酶實(shí)驗(yàn) | Briefly, transfected HEK-293 cells, incubated in charcoal-treated Dulbecco's modified Eagle's medium for 24 h, are washed once with Hanks' solution and resuspended in a buffer containing 100 mM NaCl, 1 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 250 mMsucrose, 20 mM Tris-HCl, pH 7.4. Cells are lysed by freezing in liquid nitrogen. Dehydrogenase activity is measured in a final volume of 20 μL containing the appropriate concentration of bile acid, 30 nCi of [3H]cortisol, and unlabeled cortisol to a final concentrations of 50 nM. The reaction is started by mixing cell lysate with the reaction mixture. Alternatively, endoplasmic reticulum microsomes are prepared from transfected HEK-293 cells and incubated with reaction mixture containing various concentrations of cortisol and CDCA. Incubation proceeded for 20 min, and the conversion of cortisol to cortisone is determined by thin layer chromatography (TLC). Because of the inaccuracy of the TLC method at low conversion rates and the end-product inhibition of 11βHSD2 at conversion rates higher than 60-70%, only conversion rates between 10 and 60% are considered for calculation. The inhibitory constant IC50 is evaluated using the curve-fitting program. Results are expressed as means±S.E. and consist of at least four independent measurements. |
體外活性 | Chenodeoxycholic acid (CDCA)和脫氧膽酸(DCA)均可抑制11 beta HSD2,其IC(50)值分別為22 mM和38 mM。Chenodeoxycholic acid 誘導(dǎo)皮質(zhì)醇依賴性核內(nèi)轉(zhuǎn)位,增加礦物皮質(zhì)激素受體(MR)的轉(zhuǎn)錄活性。[1] Chenodeoxycholic acid 通過(guò)激活膜G蛋白偶聯(lián)受體(TGR5)依賴性通路,顯著促進(jìn)Ishikawa細(xì)胞生長(zhǎng),增加Cyclin D1蛋白和mRNA表達(dá)。[2] 在培養(yǎng)的人類肝母細(xì)胞瘤細(xì)胞系Hep G2中,Chenodeoxycholic acid 可使LDL受體mRNA水平提高近4倍,HMG-CoA還原酶和HMG-CoA合酶mRNA水平提高2倍。[3] Chenodeoxycholic acid 誘導(dǎo)的Isc被Bumetanide、BaCl2和囊性纖維化跨膜導(dǎo)電調(diào)節(jié)器(CFTR)抑制劑CFTRinh-172抑制(≥67%)。Chenodeoxycholic acid 激活的Isc被腺苷酸環(huán)化酶抑制劑MDL12330A降低43%,Chenodeoxycholic acid 增加細(xì)胞內(nèi)cAMP濃度。[4] Chenodeoxycholic acid 通過(guò)增加其磷酸化、核內(nèi)積聚來(lái)激活C/EBPβ。Chenodeoxycholic acid 增強(qiáng)了含有C/EBP響應(yīng)元素(pGL-1651)的-1.65-kb GSTA2啟動(dòng)子結(jié)構(gòu)的熒光素酶基因轉(zhuǎn)錄。Chenodeoxycholic acid 激活A(yù)MP激活的蛋白激酶(AMPK),促進(jìn)細(xì)胞外信號(hào)調(diào)節(jié)激酶1/2(ERK1/2)的激活。[5] |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 79 mg/mL (201.23 mM) DMSO : 40 mg/mL (101.89 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | NR1H4 | Endogenous Metabolite | Inhibitor | Chenodeoxycholic acid | inhibit | Autophagy | FXR |
相關(guān)產(chǎn)品 | Glycerol | Sucrose | Hydroxychloroquine | Thymidine |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌上市藥物庫(kù) | EMA 上市藥物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 高通量篩選天然產(chǎn)物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.2651萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營(yíng)模式 | 貿(mào)易,試劑,定制,服務(wù) |
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