RQ 00203078
Chemical Name: 4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid
Purity: ≥98%
Biological Activity
RQ 00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). Exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. Reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin-induced wet dog shakes in rats. Orally active.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines.
Okamoto et al.
Int.J.Oncol., 2012;40:1431 -
Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist.
Ohmi et al.
Bioorg.Med.Chem.Lett., 2014;24:5364
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Citations for RQ 00203078
The citations listed below are publications that use Tocris products. Selected citations for RQ 00203078 include:
2 Citations: Showing 1 - 2
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Mechanoactivation of NOX2-generated ROS elicits persistent TRPM8 Ca2+ signals that are inhibited by oncogenic KRas.
Authors: Martin F Et al.
Proc Natl Acad Sci U S A 2020;117:26008-26019
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Sustained MOR Administration Induces TRPM8-Dependent Cold Hyperalgesia.
Authors: Gong and Jasmin
J Pain 2017;18:212
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