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鹅去氧胆酸钠

鹅去氧胆酸钠用途

鹅去氧胆酸钠是一种疏水性初级胆汁酸,可激活参与胆固醇代谢的核受体(FXR)。

鹅去氧胆酸钠名称

[ CAS 号 ]:
2646-38-0

[ 中文名 ]:
鹅去氧胆酸钠

[ 英文名 ]:
Sodium chenodeoxycholate

[中文别名 ]:

鹅脱氧胆酸钠

[英文别名 ]:

sodium sat of chenodeoxycholic acid
Chenodeoxycholate sodium salt
Chenodeoxycholic acid sodium
Chenodeoxycholic acid sodium salt
UNII:6V4571KSKE
sodium chenodexoycholate
5β-Cholanic acid-3α,7α-diol
sodium chenodeoxycholate
sodiumchenodesoxycholate
3α,7α-Dihydroxy-5β-cholanic acid

鹅去氧胆酸钠生物活性

[ 描述 ]:

鹅去氧胆酸钠是一种疏水性初级胆汁酸,可激活参与胆固醇代谢的核受体(FXR)。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> FXR

信号通路 >> 自噬 >> 自噬

研究领域 >> 代谢疾病

[体外研究]

鹅去氧胆酸钠(CDCA)和脱氧胆酸(DCA)均抑制11β-HSD2,IC50值分别为22 mM和38 mM,并导致皮质醇依赖性核转位,增加盐皮质激素受体(MR)的转录活性[1]。鹅去氧胆酸钠能够通过激活膜G蛋白偶联受体(TGR5)依赖性途径,诱导细胞周期蛋白D1蛋白和mRNA表达显著增加,从而刺激石川细胞生长[2]。在培养的人肝母细胞瘤细胞系Hep G2中,鹅去氧胆酸钠(CDCA)诱导LDL受体mRNA水平约为4倍,HMG-CoA还原酶和HMG-CoA合成酶的mRNA水平为2倍[3]。鹅去氧胆酸钠诱导的Isc被布美他奈、BaCl2和囊性纤维化跨膜电导调节剂(CFTR)抑制剂CFTRin-172抑制(≥67%)。腺苷酸环化酶抑制剂MDL12330A使鹅去氧胆酸钠刺激的Isc降低43%,鹅去氧胆酸盐增加细胞内cAMP浓度[4]。鹅去氧胆酸钠处理激活C/EBPβ,如其磷酸化、核积累和在HepG2细胞中表达的增加所示。鹅去氧胆酸钠增强来自含有-1.65-kb GSTA2启动子的构建体的萤光素酶基因转录,该构建体含有C/EBP应答元件(pGL-1651)。鹅去氧胆酸钠处理激活AMP活化蛋白激酶(AMPK),导致细胞外信号调节激酶1/2(ERK1/2)激活,使用AMPKα显性阴性突变体和化学抑制剂的实验结果证明了这一点[5]。

[激酶实验]

简言之，转染的HEK-293细胞在木炭处理的Dulbecco改良的Eagle培养基中孵育24小时，用Hanks溶液洗涤一次，并重悬于含有100mM NaCl、1mM MgCl2、1mM EDTA、1mM EGTA、250mM蔗糖、20mM Tris-HCl、pH 7.4的缓冲液中。细胞通过在液氮中冷冻而裂解。在含有适当浓度胆汁酸、30nCi[3H]皮质醇和最终浓度为50nM的未标记皮质醇的20μL最终体积中测量脱氢酶活性。通过将细胞裂解物与反应混合物混合来开始反应。或者，由转染的HEK-293细胞制备内质网微粒体，并与含有不同浓度皮质醇和CDCA的反应混合物孵育。培养20分钟，通过薄层色谱法（TLC）测定皮质醇向可的松的转化率。由于TLC方法在低转化率下的不准确性，以及11βHSD2在转化率高于60-70%时的最终产物抑制性，因此仅考虑10%至60%的转化率进行计算。使用曲线拟合程序来评估抑制常数IC50。结果用平均值±S.E.表示，至少由四个独立的测量值组成。

[细胞实验]

通过用相应浓度的胆汁酸孵育转染的HEK-293细胞和CHO细胞1小时并用台盼蓝染色来分析细胞活力。根据细胞增殖试剂盒I，使用四唑盐MTT（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑溴化物）分析胆汁酸的毒性。在两种测试中，对照和胆汁酸处理的细胞之间没有显著差异。

[参考文献]

[1]. Stauffer AT, et al. Chenodeoxycholic acid and deoxycholic acid inhibit 11 beta-hydroxysteroid dehydrogenase type 2 and cause cortisol-induced transcriptional activation of the mineralocorticoid receptor. J Biol Chem. 2002 Jul 19;277(29):26286-92

[2]. Noh K, et al. Farnesoid X receptor activation by chenodeoxycholic acid induces detoxifying enzymes through AMP-activated protein kinase and extracellular signal-regulated kinase 1/2-mediated phosphorylation of CCAAT/enhancer binding protein β. Drug Metab

[3]. Casaburi I, et al. Chenodeoxycholic acid through a TGR5-dependent CREB signaling activation enhances cyclin D1 expression and promotes human endometrial cancer cell proliferation. Cell Cycle. 2012 Jul 15;11(14):2699-710

[4]. Ao M, et al. Chenodeoxycholic acid stimulates Cl(-) secretion via cAMP signaling and increases cystic fibrosis transmembrane conductance regulator phosphorylation in T84 cells. Am J Physiol Cell Physiol. 2013 Aug 15;305(4):C447-56

[5]. Kawabe Y, et al. The molecular mechanism of the induction of the low density lipoprotein receptor by chenodeoxycholic acid in cultured human cells. Biochem Biophys Res Commun. 1995 Mar 8;208(1):405-11.

鹅去氧胆酸钠物理化学性质

[ 沸点 ]:
547.1ºC at 760mmHg

[ 熔点 ]:
298 °C(dec.)

[ 分子式 ]:
C₂₄H₃₉NaO₄

[ 分子量 ]:
414.55

[ 闪点 ]:
298.8ºC

[ 精确质量 ]:
414.274597

[ PSA ]:
80.59000

[ LogP ]:
3.14320

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
2.98E-14mmHg at 25°C

[ 储存条件 ]:
库房低温通风干燥

鹅去氧胆酸钠MSDS

详细MSDS(安全技术说明书)

鹅去氧胆酸钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: FZ2231000

CHEMICAL NAME :: 5-beta-Cholan-24-oic acid, 3-alpha,7-alpha-dihydroxy-, monosodium salt

CAS REGISTRY NUMBER :: 2646-38-0

LAST UPDATED :: 198508

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C24-H39-O4.Na

MOLECULAR WEIGHT :: 414.62

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,2499,1977

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1450 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from small intestine Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,2499,1977

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 114 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - acute pulmonary edema

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,2499,1977

鹅去氧胆酸钠安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H312-H332-H351

[ 警示性声明 ]:
P280-P281

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
20/21/22-40

[ 安全声明 (欧洲) ]:
S22;S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
FZ2231000

鹅去氧胆酸钠合成路线

详细合成路线

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鹅去氧胆酸钠文献

Bile acids repress hypoxia-inducible factor 1 signaling and modulate the airway immune response.

Infect. Immun. 82(9) , 3531-41, (2014)

Gastroesophageal reflux (GER) frequently occurs in patients with respiratory disease and is particularly prevalent in patients with cystic fibrosis. GER is a condition in which the duodenogastric cont...

Chenodeoxycholate in females with irritable bowel syndrome-constipation: a pharmacodynamic and pharmacogenetic analysis.

Gastroenterology 139 , 1549, (2010)

Sodium chenodeoxycholate (CDC) accelerates colonic transit in health. Our aim was to examine pharmacodynamics (colonic transit, bowel function) and pharmacogenetics of CDC in constipation-predominant ...

Bile salt/acid induction of DNA damage in bacterial and mammalian cells: implications for colon cancer.

Nutr. Cancer 16 , (1991)

Two bile salts, sodium chenodeoxycholate and sodium deoxycholate, induced a DNA repair response in the bacterium Escherichia coli. Similarly, a bile acid and a bile salt, chenodeoxycholic acid and sod...

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