GSK2193874

For research use only.

Catalog No.S8367

2 publications

GSK2193874 Chemical Structure

Molecular Weight(MW): 691.62

GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively.

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Biological Activity

Description GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively.
Targets
rTRPV4 [1]
(Cell-free assay)
hTRPV4 [1]
(Cell-free assay)
0.002 μM 0.04 μM
In vitro

GSK2193874 is profiled against TRP channels and is selective against TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8 (IC50 > 25 μM)[1]. Treatment of human umbilical vein endothelial cells (HUVECs) with GSK2193874 dose-dependently prevents the cellular contraction and detachment induced by TRPV4 activation with GSK1016790[2].

In vivo The pharmacokinetic (PK) properties for GSK2193874 are evaluated in both rat and dog and found to have half-lives and oral exposure suitable for oral dosing in chronic animal models (Rat PK: iv CL = 7.3 mL/min/kg, po t1/2 = 10 h, %F =31. Dog PK: iv CL = 6.9 mL/min/kg, po t1/2 = 31 h, %F = 53). In addition, GSK2193874 shows no blood pressure or heart rate effect in rats when dose up to 30 mg/kg. It demonstrates to has the ability to improve pulmonary functions in a number of heart failure models[1]. In both acute and chronic HF models, GSK2193874 pretreatment inhibits the formation of pulmonary edema and enhanced arterial oxygenation. TRPV4 blockade with GSK2193874 provides protection against the development of pulmonary edema and the resulting deficits in arterial oxygenation in HF models in vivo. GSK2193874 preserves endothelial cell integrity and inhibits endothelial TRPV4 currents while providing protection from formation of pulmonary edema in isolated lungs and in HF models[2].

Protocol

Cell Research:

[2]

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  • Cell lines: Stably transfected hTRPV4 HEK cells (CG27) and HUVECs
  • Concentrations: 1-30 nM(extracellularly); 0.03-10 uM(intracellularly)
  • Incubation Time: --
  • Method:

    TRPV4 HEK cells were pretreated with GSK2193874, extracellularly (1-30 nM) by application to the bathing solution, or intracellularly (0.03-10 uM) by inclusion in the pipette solution. Ramp currents were elicited between -60 and +60 mV and peak outward current at +60 mV was assessed after TRPV4 activation with GSK634775 (100 nM) added to the bath. In HUVECs, ramp currents were elicited between -80 and +80 mV and measured at + 60 mV, and the TRPV4 activator GSK1016790 (30 nM) was bath applied to activate TRPV4 followed by GSK2193874 (300 nM). 


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Adult male Sprague-Dawley rats
  • Dosages: 30 mg/kg
  • Administration: via oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (144.58 mM)
Ethanol 50 mg/mL warmed (72.29 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 691.62
Formula

C37H38BrF3N4O

CAS No. 1336960-13-4
Storage powder
in solvent
Synonyms N/A
Smiles FC(F)(F)C1=CC=CC(=C1)C2=NC3=CC(=CC=C3C(=C2CN4CCC(CC4)N5CCCCC5)C(=O)NC6(CC6)C7=CC=CC=C7)Br

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID