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. 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.
| Molecular Weight | 447.46 |
| CAS Number | 1142090-23-0 |
| Solubility (25°C) | DMSO ≥ 47 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Epoxide Hydrolase Products |
|---|
| sEH inhibitor-16
sEH inhibitor-16 is a soluble epoxide hydrolase (sEH) inhibitors with an IC50 of 2 nM. |
| UC-1728
UC-1728 is a potent rabbit soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 2 nM on rabbit liver. |
| BI-1935
BI-1935 is a potent soluble epoxide hydrolase (sEH) inhibitor. BI-1935 can be used for the research of cardiovascular disease. |
| AR-9281
AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes. |
| SWE101
SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH. |
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