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GSK2193874

GSK2193874
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Purity:98.79%
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GSK2193874

Catalog No. T5640Cas No. 1336960-13-4
GSK2193874 was identified as a selective, orally active TRPV4 blocker.
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Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$52In Stock
5 mg$74In Stock
10 mg$129In Stock
25 mg$259In Stock
50 mg$426In Stock
100 mg$633In Stock
1 mL x 10 mM (in DMSO)$113In Stock
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Product Introduction

Bioactivity
Description
GSK2193874 was identified as a selective, orally active TRPV4 blocker.
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].
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].
Chemical Properties
Molecular Weight691.62
FormulaC37H38BrF3N4O
Cas No.1336960-13-4
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 100 mg/mL (144.59 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.4459 mL7.2294 mL14.4588 mL72.2940 mL
5 mM0.2892 mL1.4459 mL2.8918 mL14.4588 mL
10 mM0.1446 mL0.7229 mL1.4459 mL7.2294 mL
20 mM0.0723 mL0.3615 mL0.7229 mL3.6147 mL
50 mM0.0289 mL0.1446 mL0.2892 mL1.4459 mL
100 mM0.0145 mL0.0723 mL0.1446 mL0.7229 mL

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