| Name | GSK1016790A |
| Description | GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells. |
| Cell Research | CPECs are treated for 20 minutes with vehicle(DMSO), 10 nM GSK, or 10 nM GSK following the pretreatment with 1 mM HC. Then the cells are fixed and stained with Coomassie Brilliant Blue.(Only for Reference) |
| In vitro | GSK1016790A elicits Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM[1]. It stimulates TRPV4 in multiple cell types including endothelial cells, urinary smooth muscle cells, urothelial cells and HEK-293 cells over-expressing TRPV4. GSK1016790A specifically activates TRPV4 channels, leading to a rapid partial desensitization and downregulation of the channel expression on the plasma membrane[2]. |
| In vivo | GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions[3]. The activation of TRPV4 by GSK1016780A leads to vasodilation, vascular leakage, and tissue hemorrhage[4]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 58 mg/mL (88.5 mM)
DMSO : 93 mg/mL (141.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | GSK1016790A | inhibit | Ca2+ channels | Inhibitor | embryonic | GSK-101 | GSK-1016790A | Ca channels | HEK | vanilloid | transient | potential | receptor | GSK 101 | TRP Channel | kidney | Calcium Channel | human | Transient receptor potential channels |
| Inhibitors Related | Nisoldipine | Nimodipine | 2,5-Di-tert-butylhydroquinone | Diltiazem hydrochloride | Levetiracetam | L-Ascorbic acid | Lanthanum(III) chloride heptahydrate | Camphor | 1,4-Cineole | Ethyl cinnamate | 1-Octanol | Otilonium bromide |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Calcium Channel Compound Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
