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G0798

Sigma-Aldrich

GSK1016790A

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

Synonyme(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

Formule empirique (notation de Hill):
C28H32Cl2N4O6S2
Numéro CAS:
942206-85-1
Poids moléculaire :
655.61
Numéro MDL:
MFCD12912413
Code UNSPSC :
12352200
ID de substance PubChem :
329799716
Nomenclature NACRES :
NA.77

product name

GSK1016790A, ≥98% (HPLC)

Pureté

≥98% (HPLC)

Forme

solid

Couleur

white

Solubilité

DMSO: >10 mg/mL

Auteur

GlaxoSmithKline

Température de stockage

−20°C

Chaîne SMILES 

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

Clé InChI

IVYQPSHHYIAUFO-VXKWHMMOSA-N

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

Actions biochimiques/physiologiques

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).

Caractéristiques et avantages

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 1

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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)
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)
Sandip M Swain et al.
The Journal of biological chemistry, 296, 100171-100171 (2020-12-11)
The ion channels Piezo1 and TRPV4 have both, independently, been implicated in high venous pressure- and fluid shear stress-induced vascular hyperpermeability in endothelial cells. However, the mechanism by which Piezo1 and TRPV4 channels execute the same function is poorly understood.
Reduced tissue osmolarity increases TRPV4 expression and pro-inflammatory cytokines in intervertebral disc cells
Walter BA, et al.
European Cells & Materials, 32, 123-123 (2016)
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