Novel, potent TRPV4 channel agonist. Induced Ca 2+ influx in mouse and human TRPV4 expressing HEK cells (EC 50 values of 18 and 2.1 nM respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ACTIVATOR
Mechanism of action
Activator of TRPV4
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells。
Associated Targets(Human)
TRPV4TchemTransient receptor potential cation channel subfamily V member 4 (4 Activities)
1.Xu S, Liu B, Yin M, Koroleva M, Mastrangelo M, Ture S, Morrell CN, Zhang DX, Fisher EA, Jin ZG. (2016) A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis.. Oncotarget, 7 (25):(37622-37635). [PMID:27191895][10.1021/op500134e]
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