Gemfibrozil 1-O-β-glucuronide
Based on 1 publication(s) in Google Scholar
Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 91683-38-4
- Formula: C21H30O9
- Molecular Weight:426.46
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Gemfibrozil 1-O-β-glucuronide
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Customer Validation & Images
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WB
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WB
Biological Activity
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CYP3 |
CYP2C8 4.07 μM (IC50) |
Gemfibrozil 1-O-β-Glucuronide significantly inhibits the OATP2 (OATP1B1)-mediated uptake of Cerivastatin (CER; HY-129458) with an IC50 of 24.3 μM[1].
Gemfibrozil 1-O-β-Glucuronide inhibits CYP2C8-mediated M1, M23 formation with IC50s of 5.38 μM, 4.30 μM, and has no effects for CYP2C8-mediated M3 formation[1].
Gemfibrozil 1-O-β-Glucuronide has an IC50 of 243 μM for the CYP3A4- mediated metabolism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 91683-38-4
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Appearance Solid
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Molecular Weight 426.46
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Formula C21H30O9
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Color White to off-white
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SMILES
O[C@H]1[C@H](OC(C(C)(C)CCCOC2=CC(C)=CC=C2C)=O)O[C@H](C(O)=O)[C@@H](O)[C@@H]1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Pachymic acid alleviates secondary lymphedema through the modulation of EETs level and the inhibition of lymphatic fibrosis. [Abstract]2025 Sep 23:162:115066. PMID: 40580744
Gemfibrozil 1-O-β-glucuronide purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115066. [Abstract]
Western blotting was used to assess fibrosis-related markers in LECs treated with Gemfibrozil 1-O-β-glucuronide, including Collagen III and α-SMA.
Gemfibrozil 1-O-β-glucuronide purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 23:162:115066. [Abstract]
CYP2C8 was detected by Western blotting in LECs treated with was treated with Gemfibrozil 1-O-β-glucuronide.
Solvent & Solubility
DMSO : 100 mg/mL (234.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Shitara Y, et al. Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2(OATP2/OATP1B1:SLC21A6)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil. J Pharmacol Exp Ther. 2004 Oct;311(1):228-36. [Content Brief]
[2]. Baer BR, et al. Benzylic oxidation of gemfibrozil-1-O-beta-glucuronide by P450 2C8 leads to heme alkylation and irreversible inhibition. Chem Res Toxicol. 2009 Jul;22(7):1298-309. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3449 mL | 11.7244 mL | 23.4489 mL | 58.6221 mL |
| 5 mM | 0.4690 mL | 2.3449 mL | 4.6898 mL | 11.7244 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3449 mL | 5.8622 mL | |
| 15 mM | 0.1563 mL | 0.7816 mL | 1.5633 mL | 3.9081 mL | |
| 20 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9311 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9380 mL | 2.3449 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9541 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4656 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9770 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL |
Gemfibrozil 1-O-β-glucuronide Related Classifications
HY-129993 Related Classifications
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