5.30533
GSK1016790A
≥98% (HPLC), powder, TRPV4 channel agonist, Calbiochem
别名:
TRPV4 Agonist, GSK1016790A, GSK101, Transient Receptor Potential Vanilloid 4 Channel Agonist
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关于此项目
经验公式（希尔记法）:
C28H32Cl2N4O6S2
化学文摘社编号:
分子量:
655.61
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
产品名称
TRPV4 Agonist, GSK1016790A,
assay
≥98% (HPLC)
Quality Segment
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
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
TRPV4
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.
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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存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable