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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

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Size/SKUAvailabilityPrice
10 mg
Please contact Customer Service for Availability
7 110,00 CZK
50 mg
Please contact Customer Service for Availability
27 900,00 CZK
23 715,00 CZK

About This Item

Empirical Formula (Hill Notation):
C28H32Cl2N4O6S2
CAS Number:
Molecular Weight:
655.61
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid

7 110,00 CZK


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Product Name

GSK1016790A, ≥98% (HPLC)

Quality Segment

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

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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This Item
616520SAB3501100EMU036101
description

≥98% (HPLC)

description

The TRPV4 Antagonist I, RN-1734, also referenced under CAS 946387-07-1, controls the biological activity of TRPV4. This small molecule/inhibitor is primarily used for Biochemicals applications.

description

affinity isolated antibody

description

targeting mouse Trpv4

form

solid

form

solid

form

buffered aqueous solution

form

lyophilized powder

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

-

assay

-

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: >10 mg/mL

solubility

DMSO: 50 mg/mL

solubility

-

solubility

-

originator

GlaxoSmithKline

originator

-

originator

-

originator

-


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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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