الصفحة الرئيسية>>Signaling Pathways>> Others>>GSK2256294A (GSK 2256294)

GSK2256294A (GSK 2256294) (Synonyms: GSK 2256294)

رقم الكتالوجGC32455

GSK2256294A (GSK 2256294) (GSK 2256294) هو مثبط انتقائي ونشط عن طريق الفم من هيدرولاز الإيبوكسيد القابل للذوبان (sEH).

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GSK2256294A (GSK 2256294) التركيب الكيميائي

Cas No.: 1142090-23-0

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
222٫00
متوفر
5mg
202٫00
متوفر
10mg
321٫00
متوفر
50mg
782٫00
متوفر
100mg
1103٫00
متوفر

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مراجعات العميل

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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 pMTarget: sEHin 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.

[1]. Podolin PL, et al. In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid Mediat. 2013 Jul-Aug;104-105:25-31.

Chemical Properties

Cas No. 1142090-23-0 SDF
المرادفات GSK 2256294
Canonical SMILES O=C([C@H]1C[C@@H](NC2=NC(NC)=NC(C)=N2)CCC1)NCC3=CC=C(C#N)C=C3C(F)(F)F
Formula C21H24F3N7O M.Wt 447.46
الذوبان DMSO : ≥ 47 mg/mL (105.04 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2348 mL 11.1742 mL 22.3484 mL
5 mM 0.447 mL 2.2348 mL 4.4697 mL
10 mM 0.2235 mL 1.1174 mL 2.2348 mL
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