Gemfibrozil 1-O-β-glucuronide

Name: Gemfibrozil 1-O-β-glucuronide
Brand: MedChemExpress
SKU: HY-129993
Rating: 4.5 (1 reviews)

Cat. No.: HY-129993 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Gemfibrozil 1-O-β-glucuronide Chemical Structure

CAS No. : 91683-38-4

Size	Price	Stock	Quantity
1 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 5280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 8450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PPAR Isoform Specific Products:

View All Isoforms

PPARα PPARβ/δ PPARγ PPAR PPARδ

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

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^[1]^[2].

IC₅₀ & Target^[1]

CYP3	CYP2C8 4.07 μM (IC₅₀)

In Vitro

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.

Molecular Weight

426.46

Formula

C₂₁H₃₀O₉

CAS No.

91683-38-4

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3449 mL	11.7244 mL	23.4489 mL
5 mM	0.4690 mL	2.3449 mL	4.6898 mL
10 mM	0.2345 mL	1.1724 mL	2.3449 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (247 KB) HNMR (217 KB) RP-HPLC (260 KB) MS (70 KB)

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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