Overview
Cat #:
R-170
Lyophilized Powder yes
Source Synthetic
MW: 554.84
Purity: >99%
Effective concentration 1 nM – 1 µM.
Structure
Chemical name 4-[[3-chloro-5-(trifluoromethyl)pyridin-2-yl]-[[4-(trifluoromethoxy)phenyl]methyl]sulfamoyl]benzoic acid.
Molecular formula C21H13ClF6N2O5S.
CAS No.: 1254205-52-1
PubChem CID 49783953
Activity RQ 00203078 is a potent and selective TRPM8 antagonist, shown to inhibit menthol-evoked human and rat TRPM8-mediated calcium influx with IC50 of 8.3 nM and 5.8 nM, respectively, while being highly selective over hTRPV4, h/rTRPV1, h/rTRPA1 and TRPM21,2.
References-Activity
- Ohmi, M. et al. (2014) Bioorg. Med. Chem. Lett. 24, 5364.
- Okamoto, Y. et al. (2012) Int. J. Oncol. 40, 1431.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at +4°C.
Solubility Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
Storage of solutions Up to three months at -20°C.
Our bioassay
Alomone Labs RQ 00203078 inhibits TRPM8 channels expressed in HEK-293 cells.Dose response curve of TRPM8 inhibition by RQ 00203078 (#R-170), showing full inhibition at 1 µM. Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of RQ 00203078, and activated by 30 nM Icilin. Changes in intracellular Ca2+ following activator application were detected as changes in 485 nm/525 nm fluorescence (RFU).
Scientific background
RQ 00203078 is a synthetic compound that acts as a potent and highly selective TRPM8 channel blocker with IC50 values of 8.3 nM and 5.8 nM for human and rat TRPM8 respectively. The compound shows very little inhibitory action against TRPV1, TRPA1, TRPV4 and TRPM2 channel. It is orally available and may be a useful tool for assessing the potential therapeutic use of TRPM81,2.
TRPM8 is a Ca2+-permeable, nonselective cation channel that is activated by temperatures in the range of 8–28°C and by chemical agonists such as menthol and icilin. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons. TRPM8 gene is up-regulated in prostate cancer and other malignancies1,3.
Target TRPM8 channel
Lyophilized Powder
For research purposes only, not for human use
Last Update: 02/01/2024
Specifications
Citations
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