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G0798

GSK1016790A

Name: GSK1016790A
Brand: SIGMA

≥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

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About This Item

Empirical Formula (Hill Notation):

C₂₈H₃₂Cl₂N₄O₆S₂

CAS Number:

942206-85-1

Molecular Weight:

655.61

UNSPSC Code:

12352200

PubChem Substance ID:

329799716

NACRES:

NA.77

MDL number:

MFCD12912413

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

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Properties

Product Name

GSK1016790A, ≥98% (HPLC)

Quality Level

100

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.

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.

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Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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When size matters: transient receptor potential vanilloid 4 channel as a volume-sensor rather than an osmo-sensor

Toft-Bertelsen TL, et al.

The Journal of Physiology, 595(11), 3287-3302 (2017)

TRPV4 channels stimulate Ca2+-induced Ca2+ release in mouse neurons and trigger endoplasmic reticulum stress after intracerebral hemorrhage

Shen J, et al.

Brain Research Bulletin, 146, 143-152 (2019)

TRPV4 regulates migration and tube formation of human retinal capillary endothelial cells

Wen L, et al.

BMC Ophthalmology, 18(1), 38-38 (2018)

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