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5.30533

Sigma-Aldrich

GSK1016790A

≥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:
Molecular Weight:
655.61
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

product name

TRPV4 Agonist, GSK1016790A,

Assay

≥98% (HPLC)

Quality Level

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

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).
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

Warning

Toxicity: Standard Handling (A)

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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