G0798

GSK1016790A

≥98% (HPLC), solid, TRPV4 channel agonist

• Synonym(s): GSK101, (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide
• Empirical Formula (Hill Notation): C₂₈H₃₂Cl₂N₄O₆S₂
• CAS Number: 942206-85-1
• Molecular Weight: 655.61
• MDL number: MFCD12912413
• UNSPSC Code: 12352200
• PubChem Substance ID: 329799716
• NACRES: NA.77

Properties

• product name: GSK1016790A, ≥98% (HPLC)
• assay: ≥98% (HPLC)
• form: solid
• color: white
• 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

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 Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable