[CAS NO. 1142090-23-0] GSK2256294A
PRODUCTS SPECIFICATIONS [1142090-23-0]
DESCRIPTION [1142090-23-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 447.46 |
| Molecular Formula | C21H24F3N7O |
| 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 |
2 Publications Citing Use of MCE
Summary
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 [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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02006537 | GlaxoSmithKline |
Pulmonary Disease, Chronic Obstructive
|
January 31, 2014 | Phase 1 |
| NCT01762774 | GlaxoSmithKline |
Pulmonary Disease, Chronic Obstructive
|
January 16, 2013 | Phase 1 |
| NCT03486223 | Vanderbilt University Medical Center|National Institutes of Health (NIH)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
Diabetes Mellitus|Endocrine System Diseases|Glucose Metabolism Disorders|PreDiabetes|Obesity
|
May 17, 2018 | Phase 2 |
| NCT03318783 | Oregon Health and Science University|Foundation for Anesthesia Education and Research|GlaxoSmithKline |
Subarachnoid Hemorrhage, Aneurysmal|Delayed Cerebral Ischemia|Vasospasm, Cerebral|Endothelial Dysfunction
|
May 2, 2018 | Phase 1|Phase 2 |
| NCT02262689 | GlaxoSmithKline|Parexel |
Pulmonary Disease, Chronic Obstructive
|
January 8, 2015 | Phase 1 |
Appearance
Solid
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
DMSO : ≥ 47 mg/mL ( 105.04 mM )
* "≥" means soluble, but saturation unknown.
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 |
