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Icosabutate 

Cat. No.: HY-121212 Purity: 97.28%
Handling Instructions

Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia .

For research use only. We do not sell to patients.

Icosabutate Chemical Structure

Icosabutate Chemical Structure

CAS No. : 1253909-57-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Liquid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 385 In-stock
Estimated Time of Arrival: December 31
Liquid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis[1]. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia [2].

IC50 & Target

IC50: non-HDL-C[2]

In Vivo

Icosabutate (oral gavage; 100 mg/kg; once) accounts for the much higher flow rate of portal vein plasma (522 mL/h) versus mesenteric lymph (0.5 mL/h), that data demonstate that icosabutate is almost entirely taken up through the portal vein (>99%) with only a small fraction of icosabutate being absorbed through the lymphatic pathway in 8‐week old male Wistar rats[1].
Icosabutate ([14‐C]‐icosabutate; oral gavage; 100 mg/kg; once) shows that peak concentrations of radioactivity in most tissues at 4‐8 hours after the dose (except the gastrointestinal tract) with highest concentrations in the liver and kidney, most other tissues contain levels of radioactivity below that in plasma in male albino Wistar rats[1].
Icosabutate (diet administration; 135 mg/kg/day; 5 weeks) markedly improved glucose tolerance after an oral glucose load, significantly reduces AUC (0‐120 minutes) by 60% without affecting body weight, decrease plasma alanine aminotransferase (ALT) levels improves glucose metabolism by a significant decrease in blood glucose, blood hemoglobin A1c, plasma insulin, and HOMA‐IR (-50%, -47%, -76% and -87%, respectively) in mice[1].
Icosabutate (oral adminstration; 112 mg/kg/day; 20 weeks) prevents microvesicular steatosis (-35%) and hepatocellular hypertrophy (-82%), but not macrovesicular steatosis. After 20 weeks of treatment, despite comparable decreases in hepatic inflammatory cell aggregates, only icosabutate reduced hepatic collagen content[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6‐8‐week‐old male ob/ob mice[1]
Dosage: 135 mg/kg
Administration: 135 mg/kg/day through diet administration; 5 weeks
Result: Improved glucose metabolism and insulin resistance.
Animal Model: 8‐15‐week‐old male APOE*3Leiden.CETP mice fed a high‐fat and high cholesterol diet[1]
Dosage: 112 mg/kg/day
Administration: Oral gavage; 20 weeks
Result: Improved microvesicular steatosis, hepatic inflammation, and fibrosis.
Clinical Trial
Molecular Weight

374.56

Formula

C24H38O3

CAS No.
SMILES

CCC(OCCCC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CC)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (266.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6698 mL 13.3490 mL 26.6980 mL
5 mM 0.5340 mL 2.6698 mL 5.3396 mL
10 mM 0.2670 mL 1.3349 mL 2.6698 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.67 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.67 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 97.28%

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Product Name:
Icosabutate
Cat. No.:
HY-121212
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