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GSK1016790A

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Purity:99.05%

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COA HPLC HNMR

GSK1016790A

Catalog No. T6848Cas No. 942206-85-1

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.

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Pack Size	Price	Availability
1 mg	$31	In Stock
2 mg	$41	In Stock
5 mg	$66	In Stock
10 mg	$115	In Stock
25 mg	$253	In Stock
50 mg	$383	In Stock
100 mg	$569	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock

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Product Introduction

Bioactivity

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.
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)
Alias	GSK101

Chemical Properties

Molecular Weight	655.61
Formula	C28H32Cl2N4O6S2
Cas No.	942206-85-1

Storage & Solubility Information

Storage

store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 58 mg/mL(88.5 mM)

DMSO: 93 mg/mL (141.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	1.5253 mL	7.6265 mL	15.2530 mL	76.2649 mL
5 mM	0.3051 mL	1.5253 mL	3.0506 mL	15.2530 mL
10 mM	0.1525 mL	0.7626 mL	1.5253 mL	7.6265 mL
20 mM	0.0763 mL	0.3813 mL	0.7626 mL	3.8132 mL
50 mM	0.0305 mL	0.1525 mL	0.3051 mL	1.5253 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0153 mL	0.0763 mL	0.1525 mL	0.7626 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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