GSK-1016790A

SKU: orb1300410

Description

GSK1016790A is a potent and selective TRPV4 channel agonist, demonstrating an EC50 of 34 nM in choroid plexus cells. This tool compound is widely used in cardiovascular, pulmonary, and renal research, facilitating the study of TRPV4's role in vitro and in animal models of edema, pain, and mechanosensation.

Research Area

Neuroscience

Key Properties

• CAS Number: 942206-85-1
• MW: 655.6
• Purity: >98%
• Formula: C₂₈H₃₂Cl₂N₄O₆S₂
• SMILES: CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N1CCN(CC1)C(=O)[C@H](CO)NS(=O)(=O)c1ccc(Cl)cc1Cl
• Target: Ion channel
• Solubility: Soluble in DMSO (up to 10 mg/ml).

Bioactivity

• Target IC50:
  TRPV4:34 nM(EC50)
• In Vivo:
  GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions. The activation of TRPV4 by GSK1016780A leads to vasodilation, vascular leakage, and tissue hemorrhage.
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• 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. 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CalciumChannel, Calcium Channel, kidney, mTRPV4, HEK, GSK 101, GSK-101, GSK1016790A, GSK-1016790A, hTRPV4, potential, vanilloid, transient, Transient receptor potential channels, TRPVChannel, TRPChannel, TRPV Channel, TRP Channel

Compound Identifiers

PubChem CID

23630211