| Name | GSK2193874 |
| Description | GSK2193874 was identified as a selective, orally active TRPV4 blocker. |
| Animal Research | Adult male Sprague-Dawley rats (n = 7 to 8 per group) were treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg/day) via oral gavage for at least 4 days before osmotic challenges.?Rats underwent acute and chronic hyper- and hypo-osmotic challenges.Sprague-Dawley (control, n = 18) and spontaneously hypertensive rats (n = 11) were implanted with Data Sciences International (DSI) radiotelemetry transmitters.?Rats were dosed with GSK2193874, and data were captured with DSI receivers and analyzed with Microsoft Excel[2]. |
| In vitro | GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents[1,2]. |
| In vivo | In isolated rodent and canine lungs, TRPV4 blockade prevented the increased vascular permeability and resultant pulmonary edema associated with elevated PVP. ?In both acute and chronic HF models, GSK2193874 pretreatment inhibited the formation of pulmonary edema and enhanced arterial oxygenation[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 81.67 mg/mL (118.09 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (5.78 mM), Sonication is recommended.
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| Keywords | TRPVChannel | TRPV4 | TRPV Channel | TRPChannel | TRP Channel | Transient receptor potential channels | Inhibitor | inhibit | GSK-2193874 | GSK2193874 | GSK 2193874 |
| Inhibitors Related | (+)-Camphor | Rosiglitazone | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Probenecid | Pregnenolone | Nonivamide | 1,4-Cineole | trans-Cinnamaldehyde | Methyl salicylate |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
