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G0798 Sigma-Aldrich

GSK1016790A

≥98% (HPLC)

Synonym: (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide, GSK101

  • CAS Number 942206-85-1

  • Empirical Formula (Hill Notation) C28H32Cl2N4O6S2

  • Molecular Weight 655.61

  •  MDL number MFCD12912413

  •  PubChem Substance ID 329799716

  •  NACRES NA.77

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Properties

Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
Quality Level   100
assay   ≥98% (HPLC)
form   white solid
solubility   DMSO: >10 mg/mL
originator   GlaxoSmithKline
storage temp.   −20°C
SMILES string   CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N3CCN(CC3)C(=O)[C@H](CO)NS(=O)(=O)c4ccc(Cl)cc4Cl
InChI   1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1
InChI key   IVYQPSHHYIAUFO-VXKWHMMOSA-N

Description

Application

GSK1016790A has been used:
• to stimulate transient receptor potential vanilloid 4 (TRPV4)-mediated currents in Xenopus laevis oocytes
• to stimulate cells in Ca2+ level measurement in human retinal capillary endothelial cells (HRCECs)
• to study the role of TRPV4 channels in brain injury after intracerebral hemorrhage (ICH)
• to trigger the opening of TRPV4 channels in bovine nucleus pulposus cells or Hanks′ Balanced Salt Solution

Packaging

10, 50 mg in glass bottle

Biochem/physiol Actions

GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 1
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Transient Receptor Potential Channels

The transient receptor potential family of ion channels consists of at least 28 mammalian members divided into six subfamilies: 7 TRPC (canonical), 6 TRPV (vanilloid), 8 TRPM (melastatin), 1 TRPA (an...
Keywords: Absorption, Apoptosis, Atomic absorption spectroscopy, Cancer, Diabetes, Endocannabinoids, Gene expression, Growth factors, Neurotransmitters, Pulsed discharge ionization detector, Respiratory, Transduction, Vitamins

Peer-Reviewed Papers
15

References

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