| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 58 mg/mL (88.47 mM), Sonication is recommended.
DMSO : 17.68 mg/mL (26.97 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.03 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | vanilloid | TRPVChannel | TRPV Channel | TRPChannel | TRP Channel | Transient receptor potential channels | transient | potential | mTRPV4 | kidney | hTRPV4 | HEK | GSK-1016790A | GSK1016790A | GSK-101 | GSK 101 | CalciumChannel | Calcium Channel |
| Inhibitors Related | Quadrol | Rosiglitazone | 2,4,6-Tri-tert-butylphenol | Caffeic Acid | Chlorocresol | L-Ascorbic acid | Probenecid | trans-Cinnamaldehyde | L-Ascorbic acid sodium salt | 2-Nitrobenzoic acid | Magnesium Chloride Hexahydrate | Magnesium sulfate |
| Related Compound Libraries | Reprogramming Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Hypertension Compound Library |
United States
