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GSK1016790A

Catalog No. T6848   CAS 942206-85-1
Synonyms: GSK101

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GSK1016790A Chemical Structure
GSK1016790A, CAS 942206-85-1
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
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Purity: 99.05%
Purity: 98.78%
Purity: 96.25%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

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)

TargetMolReferences and Literature

1. Thorneloe KS, et al. J Pharmacol Exp Ther. 2008, 326(2):432-42. 2. Jin M, et al. PLoS One. 2011, 6(2):e16713. 3. Pankey EA, et al. Am J Physiol Heart Circ Physiol. 2014, 306(1):H33-40. 4. Narita K, et al. FASEB J. 2015, 29(6):2247-59.

TargetMolCitations

1. Zheng Q, Zou Y, Teng P, et al. Mechanosensitive Channel PIEZO1 Senses Shear Force to Induce KLF2/4 Expression via CaMKII/MEKK3/ERK5 Axis in Endothelial Cells. Cells. 2022, 11(14): 2191 2. Kong S, Chen T, Jia X, et al.Cell-specific NFIA upregulation promotes epileptogenesis by TRPV4-mediated astrocyte reactivity.Journal of Neuroinflammation.2023, 20(1): 1-22.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library Bioactive Compounds Library Max Metabolism Compound Library Anti-Cancer Compound Library Bioactive Compound Library Anti-Hypertension Compound Library Anti-Cardiovascular Disease Compound Library Reprogramming Compound Library Neuronal Signaling Compound Library Calcium Channel Compound Library

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Keywords

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

 

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