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GSK2256294A (Synonyms: GSK 2256294)

Cat. No.: HY-19644 Purity: 99.35%
Handling Instructions

GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.

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
10 mM * 1 mL in DMSO USD 290 In-stock
Estimated Time of Arrival: December 31
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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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH. IC50 value: 27 pM Target: sEH in vitro: GSK2256294A also displays potent cellular inhibition (IC50 = 0.66 nM) of sEH in an assay developed using a cell line transfected with the human sEH enzyme. [1] in vivo: A novel, potent, selective inhibitor of recombinant human, rat and mouse sEH, GSK2256294A, exhibits potent cell-based activity, a concentration-dependent inhibition of the conversion of 14,15-EET to 14,15-DHET in human, rat and mouse whole blood, and a dose-dependent increase in the LTX/LTX diol ratio in rat plasma following oral administration. Mice receiving 10 days of cigarette smoke exposure concomitant with oral administration of GSK2256294A exhibits significant, dose-dependent reductions in pulmonary leukocytes and keratinocyte chemoattractant levels. Mice receiving oral administration of GSK2256294A following 10 days of cigarette smoke exposure exhibited significant reductions in pulmonary leukocytes compared to vehicle-treated mice.

Clinical Trial
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.
References
Molecular Weight

447.46

Formula

C₂₁H₂₄F₃N₇O

CAS No.

1142090-23-0

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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

Cat. No.: HY-19644