| 产品详情 |
| Edit |   |
|---|
| Product Name | GW 848687X |
|---|
| Description | Purity >97%. Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via G alpha q to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM). It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM). It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels. Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species. In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg. |
|---|
| Size | n/a |
|---|
| Concentration | n/a |
|---|
| Applications | n/a |
|---|
| Other Names | 6-[2-[5-chloro-2-[(2,4-digluorophenyl)methoxy]phenyl]-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid |
|---|
| Gene, Accession, CAS # | CAS: 612831-24-0 |
|---|
| Catalog # | LS-H50 |
|---|
| Price | |
|---|
| Order / More Info | GW 848687X from LIFESPAN BIOSCIENCES INC. |
|---|
| Product Specific References | n/a |
|---|
| 产品资料 |
|
|