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Lithocholic Acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lithocholic Acid图片
CAS NO:434-13-9
规格:≥98%
包装与价格:
包装价格(元)
1g电议
2g电议
5g电议
10g电议
50g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)376.57
FormulaC24H40O3
CAS No.434-13-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 75 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 47 mg/mL (124.8 mM)
Other info
Chemical Name: 3alpha-Hydroxy-5beta-cholan-24-oic acid
InChi Key: SMEROWZSTRWXGI-HVATVPOCSA-N
InChi Code: InChI=1S/C24H40O3/c1-15(4-9-22(26)27)19-7-8-20-18-6-5-16-14-17(25)10-12-23(16,2)21(18)11-13-24(19,20)3/h15-21,25H,4-14H2,1-3H3,(H,26,27)/t15-,16-,17-,18+,19-,20+,21+,23+,24-/m1/s1
SMILES Code: C[C@H](CCC(O)=O)[C@H]1CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C
SynonymsLithocolic acid; Lithocholate; 3α-Hydroxy-5β-cholanic acid
实验参考方法
In Vitro

In vitro activity: 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 is a ligand for 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


Kinase Assay: 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.

In VivoAdministration 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.
Animal modelMice
Formulation & DosageDissolved in Corn oil; 125 mg/kg; i.p. injection
ReferencesProc Natl Acad Sci U S A. 2001 Mar 13;98(6):3369-74; Science. 2002 May 17;296(5571):1313-6.