Dehydrolithocholic Acid
(Synonyms: 3-Ketolithocholic Acid) 目录号 : GC47182A major metabolite of lithocholic acid
Cas No.:1553-56-6
Sample solution is provided at 25 µL, 10mM.
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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)
| Cas No. | 1553-56-6 | SDF | |
| 别名 | 3-Ketolithocholic Acid | ||
| 化学名 | (5β)-3-oxo-cholan-24-oic acid | ||
| Canonical SMILES | C[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 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6695 mL | 13.3476 mL | 26.6951 mL |
| 5 mM | 0.5339 mL | 2.6695 mL | 5.339 mL |
| 10 mM | 0.267 mL | 1.3348 mL | 2.6695 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet