store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 31.00 | |
2 mg | In stock | $ 41.00 | |
5 mg | In stock | $ 66.00 | |
10 mg | In stock | $ 115.00 | |
25 mg | In stock | $ 253.00 | |
50 mg | In stock | $ 383.00 | |
100 mg | In stock | $ 569.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 98.00 |
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. |
Targets&IC50 | TRPV4:34 nM(EC50) |
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]. |
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) |
Synonyms | GSK101 |
Molecular Weight | 655.61 |
Formula | C28H32Cl2N4O6S2 |
CAS No. | 942206-85-1 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 58 mg/mL(88.5 mM)
DMSO: 93 mg/mL (141.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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GSK1016790A 942206-85-1 Membrane transporter/Ion channel Metabolism Calcium Channel TRP/TRPV Channel inhibit Ca2+ channels Inhibitor embryonic GSK-101 GSK-1016790A Ca channels HEK vanilloid transient potential receptor GSK 101 TRP Channel kidney GSK101 human Transient receptor potential channels inhibitor