1. Metabolic Enzyme/Protease
  2. Epoxide Hydrolase
  3. GSK2256294A

GSK2256294A  (Synonyms: GSK 2256294)

Cat. No.: HY-19644 Purity: 99.53%
COA Handling Instructions

GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease.

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

GSK2256294A Chemical Structure

GSK2256294A Chemical Structure

CAS No. : 1142090-23-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 290 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 290 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease[1].

IC50 & Target

IC50: 27 pM (recombinant human sEH), 61 pM (rat sEH orthologs), 189 pM (murine sEH orthologs)[1]

In Vitro

GSK2256294A (300 pM-10 μM; 2 h) inhibits the conversion of 14,15-EET-d11 to 14,15-DHET-d11 in human, rat and mouse whole blood[1].

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

In Vivo

GSK2256294A (5-30 mg/kg; p.o. twice daily 5 days/week for two weeks) inhibits the generation and maintenance of pulmonary inflammation in cigarette smoke-exposed mice[1].
GSK2256294A (30 mg/kg; p.o. twice daily for 8 days) decreases pulmonary inflammation in cigarette smoke-exposed mice[1].

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

Animal Model: Mice exposed to cigarette smoke 5 days/week for 2 weeks[1]
Dosage: 5 and 30 mg/kg
Administration: Oral gavage; 5 and 30 mg/kg twice daily 5 days/week; for 2 weeks
Result: Dose-dependently inhibited numbers of BAL fluid total cells, neutrophils, macrophages and the keratinocyte chemoattractant (KC) levels in lung tissue.
Animal Model: Mice exposed to cigarette smoke 5 days/week for 2 weeks[1]
Dosage: 30 mg/kg
Administration: Oral gavage; 30 mg/kg twice daily; for 8 days
Result: Significantly reduced neutrophils, macrophages and pulmonary inflammation in cigarette smoke-exposed mice.
Clinical Trial
Molecular Weight

447.46

Formula

C21H24F3N7O

CAS No.
SMILES

O=C([[email protected]]1C[[email protected]@H](NC2=NC(NC)=NC(C)=N2)CCC1)NCC3=CC=C(C#N)C=C3C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (105.04 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2348 mL 11.1742 mL 22.3484 mL
5 mM 0.4470 mL 2.2348 mL 4.4697 mL
10 mM 0.2235 mL 1.1174 mL 2.2348 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: ≥ 2.08 mg/mL (4.65 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.53%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GSK2256294A
Cat. No.:
HY-19644
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