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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G655175-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $290.90 |
Specifications & Purity | 10mM in DMSO |
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Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product 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 IC 50 s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease 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. 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 . GSK2256294A (30 mg/kg; p.o. twice daily for 8 days) decreases pulmonary inflammation in cigarette smoke-exposed mice . 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 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 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. IC50& Target:IC50: 27 pM (recombinant human sEH), 61 pM (rat sEH orthologs), 189 pM (murine sEH orthologs) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Canonical SMILES | CC1=NC(=NC(=N1)NC2CCCC(C2)C(=O)NCC3=C(C=C(C=C3)C#N)C(F)(F)F)NC |
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Molecular Weight | 447.46 |
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