GlpBio

Lithocholic Acid

目录号: GC17057纯度: >98.00%同义词: 石胆酸; 3α-Hydroxy-5β-cholanic acid
A toxic secondary bile acid
Lithocholic Acid
Cas No.: 434-13-9
规格价格库存数量操作
500mg¥280.00现货
1
1g¥420.00现货
1
5g¥672.00现货
1
10mM (in 1mL DMSO)¥350.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

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产品描述 Description

Lithocholic acid (LCA) is a toxic secondary bile acid, causing intrahepatic cholestasis, which has tumor-promoting activity.

In vitro: Among 17 kinds of bile acids with respect to inhibition of mammalian DNA polymerases, only LCA and its derivatives inhibited DNA polymerases, while other bile acids did not show inhibitory effect [1].

In vivo: Administration of LCA and its conjugates to rodents causes intrahepatic cholestasis, which is a pathogenic state characterized by decreased bile flow and the accumulation of bile constituents in the liver and blood [2].

Clinical trials: Currently no clinical data are available.

References:
[1] Ogawa A, Murate T, Suzuki M, Nimura Y, Yoshida S.  Lithocholic acid, a putative tumor promoter, inhibits mammalian DNA polymerase beta. Jpn J Cancer Res. 1998 Nov;89(11):1154-9.
[2] Staudinger JL, Goodwin B, Jones SA, Hawkins-Brown D, MacKenzie KI, LaTour A, Liu Y, Klaassen CD, Brown KK, Reinhard J, Willson TM, Koller BH, Kliewer SA.  The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3369-74.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

HL-1 cells

Preparation method

The solubility of this compound in DMSO is > 13 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

50 or 100 μM

Applications

In HL-1 cells, Lithocholic Acid reduced and prevented cardiomyocyte apoptosis at the concentrations of 50 and 100 μM, respectively. In the presences of the pro-apoptotic stimulus, Doxazosin, Lithocholic Acid inhibited hyperphosphorylation of EphA2. In addition, Lithocholic Acid increased the expression of total EphA2.
Animal experiment [2]:

Animal models

Mice

Dosage form

0.125 mg/g; i.p.; b.i.d., for 4 days.

Applications

In PXR-/- mice, Lithocholic Acid resulted in sticky residues. Analysis of the urine revealed that PXR-/- mice showed substantially increased levels of Lithocholic Acid compared with wild-type animals. In addition, wild-type mice treated with Lithocholic Acid in a shorter term showed significant increases in hepatic Cyp3a11 and Oatp2 expression, whereas Lithocholic Acid treatment exhibited no effect on the expression of those genes in PXR-/- mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Jehle J, Staudacher I, Wiedmann F, Schweizer P, Becker R, Katus H, Thomas D. Regulation of apoptosis in HL-1 cardiomyocytes by phosphorylation of the receptor tyrosine kinase EphA2 and protection by lithocholic acid. Br J Pharmacol. 2012 Dec;167(7):1563-72.

[2]. Staudinger JL, Goodwin B, Jones SA, Hawkins-Brown D, MacKenzie KI, LaTour A, Liu Y, Klaassen CD, Brown KK, Reinhard J, Willson TM, Koller BH, Kliewer SA. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3369-74.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
434-13-9
同义词
石胆酸; 3α-Hydroxy-5β-cholanic acid
化学名
(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
SMILES
CC(CCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C
分子式
C24H40O3
分子量
376.57 g/mol
溶解性
≥ 12.95mg/mL in DMSO
保存条件
Store at 4°C
General tips
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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol