Raloxifene 4'-Glucuronide
(Synonyms: 雷洛昔芬-4'-葡萄糖醛酸苷) 目录号 : GC44804
A metabolite of raloxifene
Cas No.:182507-22-8
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
Raloxifene 4'-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene . It is formed from raloxifene via the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1, UGT1A8, and UGT1A10. It binds to the estrogen receptor with an IC50 value of 370 nM. Raloxifene 4'-glucuronide inhibits the voltage-gated potassium channel Kv4.3 by 6.2 and 20.1% when used at concentrations of 10 and 30 µM, respectively.
| Cas No. | 182507-22-8 | SDF | |
| 别名 | 雷洛昔芬-4'-葡萄糖醛酸苷 | ||
| Canonical SMILES | OC1=CC=C(C(C(C2=CC=C(OCCN3CCCCC3)C=C2)=O)=C(C4=CC=C(O[C@@H]5O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]5O)C=C4)S6)C6=C1 | ||
| 分子式 | C34H35NO10S | 分子量 | 649.7 |
| 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 | 1.5392 mL | 7.6959 mL | 15.3917 mL |
| 5 mM | 0.3078 mL | 1.5392 mL | 3.0783 mL |
| 10 mM | 0.1539 mL | 0.7696 mL | 1.5392 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。
The role of pH in the glucuronidation of raloxifene, mycophenolic acid and ezetimibe
Mol Pharm 2009 Jul-Aug;6(4):1216-27.PMID:19449843DOI:10.1021/mp900065b.
The UDP-glucuronosyltransferase (UGT) active site faces the lumen of the endoplasmic reticulum and is enclosed behind a lipid bilayer. Consequently, observed UGT activity is latent in microsomal preparations, and thus, mechanical and/or chemical disruptions of the vesicle membrane are commonly employed to better expose the active site. The aim of the present investigation was to explore the impact of incubation pH on the glucuronidation of raloxifene, mycophenolic acid (MPA) and ezetimibe, which are basic, acidic and neutral compounds, respectively. Their glucuronidation was examined in human liver microsomal incubations by monitoring for the production of the glucuronide metabolites at pHs ranging between 5.4 and 9.4. Compared to physiological pH, unbound intrinsic clearance (CL(int,u)) was 11- and 12-fold higher at pH 9.4 for Raloxifene 4'-Glucuronide (R4G) and raloxifene 6-glucuronide (R6G), respectively; whereas a 10-fold increase was observed at pH 5.4 for MPA glucuronide (MPAG). In contrast, ezetimibe glucuronidation did not vary as the pH deviated from 7.4. Kinetic analysis revealed that increases in CL(int,u) were accompanied by less than a 2-fold change in V(max). Instead, K(m,u) decreased 8-, 13- and 5-fold for R4G, R6G and MPAG, respectively. Similar pH dependency on glucuronidation was observed in experiments utilizing recombinant UGT enzymes (recUGT). Particularly, recUGT1A9 was one of the major isoforms involved in the glucuronidation of raloxifene and MPA. While the highest rate of glucuronidation was found at pH 9.4 for raloxifene, the pH for optimal glucuronidation of MPA was between 5.4 and 7.4. In summary, these results suggest that microsomal glucuronidation may be enhanced for acidic and basic compounds by altering the incubation pH, perhaps by improving substrate membrane permeability.