Description: Potent and selective TRPV4 antagonist
Chemical Name:N-[4-[[4-(1-Methylethyl)-1-piperazinyl]sulfonyl]phenyl]-2-nitro-4-(trifluoromethyl)benzamide hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective TRPV4 antagonist (IC50 values are 320, 420 and 660 nM for mouse, human and rat channels, respectively). Exhibits >15-fold selectivity for TRPV4 over TRPV1, TRPV3 and TRPM8, and a panel of 54 other common biological targets. Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
53.69
100
Preparing Stock Solutions
The following data is based on the product molecular weight 536.95. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.86 mL
9.31 mL
18.62 mL
5 mM
0.37 mL
1.86 mL
3.72 mL
10 mM
0.19 mL
0.93 mL
1.86 mL
50 mM
0.04 mL
0.19 mL
0.37 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Weiet al (2015) Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg.Med.Chem.Lett. 25 4011 PMID: 26235950