GSK2193874

Catalog No.S8367

For research use only.

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.

GSK2193874 Chemical Structure

CAS No. 1336960-13-4

Selleck's GSK2193874 has been cited by 5 Publications

Purity & Quality Control

Choose Selective TRP Channel Inhibitors

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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 M1rSbGZ2dmO2aX;uJIF{e2G7 NHjtfJIyOCCvaX7z MoPGRY51[WexbnnzeEBi[3Srdnn0fUBifCC{YYSgWHJRXjRiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEeVS{[zOFc4PUFvaX7keYNm\CClYXzjbZVuKGmwZnz1fEBxemWrbnP1ZoF1\WRiZn;yJFExKG2rboOg[o9tdG:5ZXSgZpkhT1ONNkO0O|c2SSCjZHTpeIlwdiCkeTDGeZJiNTRiZInlJIJie2WmIF\MTXBTKGG|c3H5MEBKSzVyPUCuNFAz|ryP M3LNT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUKzNVA6Lz5{OEWyN|ExQTxxYU6=
HEK293 MnL4SpVv[3Srb36gZZN{[Xl? NHnxT4kyOCCvaX7z NWn1PYJSSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCWUmDWOEBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS3NMPjN2N{e1RU1qdmS3Y3XkJINidGOrdX2gbY5ndHW6IIDy[Ylv[3WkYYTl[EBnd3JiMUCgcYlveyCob3zsc5dm\CCkeTDHV2s3OzR5N{XBJIFl\Gm2aX;uJIJ6KE[3cnGtOEBlgWViYnHz[YQhTkyLUGKgZZN{[XluIFnDOVA:OC5yNN88US=> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV{M{GwPUc,Ojh3MkOxNFk9N2F-
HEK NH\EU3dHfW6ldHnvckBie3OjeR?= MoLhRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBVWlCYNDDjbIFvdmWuIITyZY5{\mWldHXkJIlvKEiHSzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEeVS{[zOFc4PS2ndn;r[YQhS2F{KzDpcoZtfXhiYomgSmxKWFJibXX0bI9lNCCLQ{WwQVAvODUQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV|Mk[2Nkc,OzF3M{K2OlI9N2F-
HEK MWHGeY5kfGmxbjDhd5NigQ>? MUXBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHRTWFZ2IHX4dJJme3OnZDDpckBJTUtiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBIW0t4M{S3O|UucW6mdXPl[EBE[TJtIHnu[ox2gCCkeTDGUGlRWiCjc4PhfUwhUUN3ME2wMlA2|ryP MnjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3MECxPVAoRjNyNUCwNVkxRC:jPh?=
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 (from reference)

Cell Research:

[2]

  • 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). 

Animal Research:

[2]

  • Animal Models: Adult male Sprague-Dawley rats
  • Dosages: 30 mg/kg
  • Administration: via oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 691.62
Formula

C37H38BrF3N4O

CAS No. 1336960-13-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(CC1)C2CCN(CC2)CC3=C(C4=C(C=C(C=C4)Br)N=C3C5=CC(=CC=C5)C(F)(F)F)C(=O)NC6(CC6)C7=CC=CC=C7

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Tech Support

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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