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Etofibrate

Alias: Etofibrate
Cat No.:V1967 Purity: ≥98%
Etofibrate, the ethandiol-1,2 diester of the nicotinic and clofibric acid, is a combination of conjugated clofibrate and niacin that is used to treat hyperlipemia.
Etofibrate
Etofibrate Chemical Structure CAS No.: 31637-97-5
Product category: Others
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Etofibrate, the ethandiol-1,2 diester of the nicotinic and clofibric acid, is a combination of conjugated clofibrate and niacin that is used to treat hyperlipemia. Etofibrate treatment heightens the cytosolic glycerol-3-phosphate dehydrogenase activity and the total carnitine concentration in the liver of rats, whereas it reduces triacylglycerol and cholesterol concentrations. Etofibrate decreases plasma levels of cholesterol, triacylglycerols, free fatty acids (FFA) and glycerol, as well as the total and unesterified cholesterol concentrations, in liver microsomes of rats.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Etofibrate treatment heightens the cytosolic glycerol-3-phosphate dehydrogenase activity and the total carnitine concentration in the liver of rats, whereas it reduces triacylglycerol and cholesterol concentrations. Etofibrate decreases plasma levels of cholesterol, triacylglycerols, free fatty acids (FFA) and glycerol, as well as the total and unesterified cholesterol concentrations, in liver microsomes of rats. Etofibrate increases the activity of liver cytosolic glycerol-3-P dehydrogenase in the rats, whereas it decreases the activity of both microsomal HMG-CoA reductase and cholesterol 7 alpha-hydroxylase and does not affect acyl-CoA: cholesterol acyltransferase (ACAT). Etofibrate decreases the availability of lipolytic products in the liver by acting on their release from adipose tissue and on their intrinsic hepatic metabolism. Etofibrate stimulates the rate of fatty acid re-esterification when incubations are done under basal conditions in epididymal fat pad pieces from fed rats.

ln Vivo
The ethandiol-1,2 diester of nicotinic and clofibric acids is called etofibrate. Both in humans and animals, etofibrate has demonstrated to be a highly effective hypolipidemic medication. Following a 10-day Etofibrate treatment period, the rats' body weight is comparable to that of the control group, but their liver weight has dramatically increased while their levels of triacylglycerol and plasma cholesterol have dropped. When the enterohepatic circulation is interrupted, etofibrate administration causes the animals' bile flow to rise. This effect is most noticeable during the first two hours, and after 30 and 90 minutes, the difference with the controls is statistically significant. Rats treated with Etofibrate and control groups exhibit a highly significant linear association in the cumulative amount of bile secreted plotted against time, with the Etofibrate group's slope being much higher than the control group's[1].
Animal Protocol
Male Sprague Dawley rats weighing 200 to 220 g, fed ad libitum a standard laboratory diet and subjected to a 12 hr on-off light cycle and 22 to 24°C are used. Food is removed from the cages at the onset of the light cycle (7.00 a.m.) and 3 hr later, Etofibrate is administered by stomach tube without anesthesia at a dose of 300 mg/kg body weight/day to one group of animals whereas another, control, group is treated with the medium. After treatments, rats are again allowed free access to food. On the 10th day, the animals are treated as above, but 2 hr after receiving the Etofibrate or the medium the rats are anesthetized with an intraperitoneal injection (0.30 mL/100 g body weight). Animals are maintained at 37°C in a thermostatically controlled cabinet
Male Sprague Dawley rats
References
[1]. Bocos C, et al. Effect of etofibrate on bile production in the normolipidemic rat. Gen Pharmacol. 1995 May;26(3):537-42
Additional Infomation
Etofibrate is a monocarboxylic acid.
Etofibrate is a fibrate produced by the combination of clofibrate ester linked to niacin. These components separate in the body slowly allowing for pharmacokinetics similar to controlled-release formulations.
Etofibrate is an orally-available combination of clofibrate and niacin linked together by an ester bond. In the body clofibrate and niacin separate, acting as a controlled-release formulation.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H18CLNO5
Molecular Weight
363.79
Exact Mass
363.087
CAS #
31637-97-5
Related CAS #
31637-97-5
PubChem CID
65777
Appearance
Typically exists as solid at room temperature
Density
1.3±0.1 g/cm3
Boiling Point
486.8±35.0 °C at 760 mmHg
Melting Point
42-44ºC
Flash Point
248.2±25.9 °C
Vapour Pressure
0.0±1.2 mmHg at 25°C
Index of Refraction
1.555
LogP
3.15
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
9
Heavy Atom Count
25
Complexity
449
Defined Atom Stereocenter Count
0
SMILES
O=C(C1=CC=CN=C1)OCCOC(C(C)(OC2=CC=C(Cl)C=C2)C)=O
InChi Key
XXRVYAFBUDSLJX-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H18ClNO5/c1-18(2,25-15-7-5-14(19)6-8-15)17(22)24-11-10-23-16(21)13-4-3-9-20-12-13/h3-9,12H,10-11H2,1-2H3
Chemical Name
2-[2-(4-Chlorophenoxy)-2-methylpropanoyl]oxyethyl pyridine-3-carboxylate
Synonyms
Etofibrate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:73 mg/mL (200.7 mM)
Water:<1 mg/mL
Ethanol:73 mg/mL (200.7 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7488 mL 13.7442 mL 27.4884 mL
5 mM 0.5498 mL 2.7488 mL 5.4977 mL
10 mM 0.2749 mL 1.3744 mL 2.7488 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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