Glyco-Obeticholic Acid
(Synonyms: 奥贝胆酸杂质8) 目录号 : GC45466
An active metabolite of obeticholic acid
Cas No.:863239-60-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Glyco-obeticholic acid is an active metabolite of obeticholic acid, which is a farnesoid X receptor (FXR) agonist and semisynthetic derivative of chenodeoxycholic acid .1 Glyco-obeticholic acid is formed from obeticholic acid by glycine conjugation in the liver but can be reconverted back to obeticholic acid by microorganism-mediated deconjugation in the ileum and colon. It has been used as a precursor in the synthesis of bile acid analogs as agonists of the farnesoid X receptor (FXR) and TGR5.2
References
1. Markham, A., and Keam, S.J. Obeticholic Acid: First global approval. Drugs 76(12), 1221-1226 (2016).
| Cas No. | 863239-60-5 | SDF | |
| 别名 | 奥贝胆酸杂质8 | ||
| Canonical SMILES | CC[C@@H]1[C@]2([H])C[C@H](O)CC[C@]2(C)[C@]3([H])[C@@]([C@@](CC[C@]4([H])[C@@H](CCC(NCC(O)=O)=O)C)([H])[C@]4(C)CC3)([H])[C@@H]1O | ||
| 分子式 | C28H47NO5 | 分子量 | 477.7 |
| 溶解度 | DMSO: slightly soluble,Methanol: slightly soluble | 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 | 2.0934 mL | 10.4668 mL | 20.9336 mL |
| 5 mM | 0.4187 mL | 2.0934 mL | 4.1867 mL |
| 10 mM | 0.2093 mL | 1.0467 mL | 2.0934 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。
A novel LC-MS/MS method for simultaneous estimation of obeticholic acid, Glyco-Obeticholic Acid, tauro-obeticholic acid in human plasma and its application to a pharmacokinetic study
J Sep Sci 2021 Apr;44(7):1307-1323.PMID:33395497DOI:10.1002/jssc.202001050
A rapid, robust, simple, selective, and sensitive liquid chromatography-tandem mass spectrometry method was developed for the simultaneous estimation of obeticholic acid and its two pharmacologically active metabolites, Glyco-Obeticholic Acid, and tauro-obeticholic acid in human plasma. The analytes and their heavy stable isotope-labeled internal standards were extracted from 250 μL human plasma by a solid-phase extraction technique. The method linearity was established over a concentration range of 0.410 to 120.466 ng/mL for obeticholic acid, 0.414 to 121.708 ng/mL for Glyco-Obeticholic Acid, and 0.255 to 75.101 ng/mL for tauro-obeticholic acid. The method was fully validated as per current guidelines on bioanalytical method validation of "United States of Food and Drug Administration" and "European Medicines Agency." The method was successfully applied to study the pharmacokinetics of obeticholic acid, Glyco-Obeticholic Acid, and tauro-obeticholic acid following oral administration of obeticholic acid tablets to healthy male volunteers. All the measured concentrations were within calibration curve ranges.