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5.30533

GSK1016790A

Name: GSK1016790A
Brand: MM

≥98% (HPLC), powder, TRPV4 channel agonist, Calbiochem

Synonym(s):

TRPV4 Agonist, GSK1016790A, GSK101, Transient Receptor Potential Vanilloid 4 Channel Agonist

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About This Item

Empirical Formula (Hill Notation):

C₂₈H₃₂Cl₂N₄O₆S₂

CAS Number:

942206-85-1

Molecular Weight:

655.61

UNSPSC Code:

12352200

NACRES:

NA.77

PubChem Substance ID:

23630211

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

Product Name

TRPV4 Agonist, GSK1016790A,

assay

≥98% (HPLC)

Quality Level

100

form

powder

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 50 mg/mL

storage temp.

−20°C

SMILES string

CC(C)CC(C(=O)N1CCN(CC1)C(=O)C(CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3

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)

InChI key

IVYQPSHHYIAUFO-UHFFFAOYSA-N

Description

General description

A cell-permeable piperazine amide derivative that acts as a potent and selective agonist of Transient Receptor Potential Vanilloid 4 Channel (TRPV4) and enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM and 18 nM in human and mouse TRPV4 expressed in HEK293 cells, respectively). Generates greater [Ca2+]i transients in chrondocytes than hypoosmotic treatments. Shown to be about 300-fold more potent that 4-α-PDD in activating TRPV4 channels. Suggested to act by recruiting previously inactive channels, rather than through increasing elevation of basal activity. Does not affect TRPM8 and TRPA1 channels even at high concentrations (~20 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Primary Target
TRPV4

Packaging

Packaged under inert gas

Other Notes

OʹConor, C.J., 2014. PNAS.111, 1316.
Sullivan, M.N., et al. 2012. Mol. Pharmacol.82, 464.
Jun, M., et al. 2011. PLoS One.6, e16713.
Thorneloe, K. S., et al. 2008. J. Pharm. Exp. Ther.326,432.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c