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Dehydrolithocholic 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。
Dehydrolithocholic Acid图片
CAS NO:1553-56-6
包装与价格：
包装价格(元)
10mg电议
50mg电议
100mg电议
250mg电议

产品介绍
Dehydrolithocholic Acid (Dehydrolithocholic acid) 是一种胆汁酸代谢物，通过直接结合关键转录因子 RORγt (Kd=1.13 μM) 来抑制 TH17 细胞的分化。
Cas No.1553-56-6
别名3-Ketolithocholic Acid
化学名(5β)-3-oxo-cholan-24-oic acid
Canonical SMILESC[C@H](CCC(O)=O)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC[C@]4([H])CC(CC[C@]4(C)[C@@]3([H])CC[C@@]21C)=O
分子式C24H38O3
分子量374.6
溶解度DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml,DMSO: 15 mg/ml,Ethanol: 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dehydrolithocholic acid is a major metabolite of lithocholic acid .[1] It is formed from LCA by the cytochrome P450 (CYP) isoform CYP3A4. Dehydrolithocholic acid is an agonist of G protein-coupled bile acid activated receptor 1 (GP-BAR1/TGR5; EC50 = 0.27 μM), vitamin D receptor (VDR; EC50 = 3 μM), and farnesoid X receptor (FXR) in cell-based reporter assays.[2],[3] It also binds to the human pregnane X receptor (PXR; IC50 = 15 μM) and activates mouse and human PXRs in cell-based reporter assays when used at a concentration of 100 μM.[4] Dehydrolithocholic acid binds to retinoic acid receptor-related orphan receptor γt (RORγt; Kd = 1.13 μM for the recombinant human ligand-binding domain) and decreases its activity in a cell-based reporter assay when used at a concentration of 10 μM.[5] It inhibits the differentiation of T helper cells that express IL-17a (TH17 cells) when used at a concentration of 20 μM.

Reference:
[1].Deo, A.K., and Bandiera, S.M.3-Ketocholanoic acid is the major in vitro human hepatic microsomal metabolite of lithocholic acidDrug Metab. Dispos.37(9)1938-1947(2009)
[2].Sato, H., Macchiarulo, A., Thomas, C., et al.Novel potent and selective bile acid derivatives as TGR5 agonists: Biological screening, structure-activity relationships, and molecular modeling studiesJ. Med. Chem.51(6)1831-1841(2008)
[3].Makishima, M., Lu, T.T., Xie, W., et al.Vitamin D receptor as an intestinal bile acid sensorScience296(5571)1313-1316(2002)
[4].Staudinger, J.L., Goodwin, B., Jones, S.A., et al.The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicityProc. Natl. Acad. Sci. USA98(6)3369-3374(2000)
[5].Hang, S., Paik, D., Yao, L., et al.Bile acid metabolites control TH17 and Treg cell differentiationNature576(7785)143-148(2019)