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Medchemexpress LLC N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide | 942206-85-1 | 99.9% | 655.61 | 1 ML
SDP

Supplier:  Medchemexpress LLC HY1960810MM/1ML

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GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. It can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells.

  • GSK1016790A (0.1-1000 nM) elicits Ca2+ influx in mouse and human TRPV4-expressing human embryonic kidney (HEK) cells (EC50 values of 18 and 2.1 nM, respectively) and it evokes a dose-dependent activation of whole-cell currents at concentrations above 1 nM.
  • GSK1016790A (100 nM) treatment elicits a rapid elevation of intracellular Ca2+ in a subset of neurons.
  • GSK1016790A (0.001-0.1 mg/kg; i.p.) produces a dose-dependent inhibitory effect on whole gut transit time in mice.
  • GSK1016790A (0.1-1000 nM; pretreatment 10 min) significantly inhibits the electrical field stimulation (EFS)-induced twitch contractions in isolated mouse colon strips in a concentration-dependent manner.

Catalog No. 50-004-00477


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