RQ 00203078

Name RQ 00203078
Supplier Tocris Bioscience
Catalog 5524
Prices $185.00, $755.00
Sizes 10 mg, 50 mg
Function Type Antagonist
Cas Number 1254205-52-1
Chemical Name 4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoicacid
Formula C21H13ClF6N2O5S
Molecular Weight 554.85
Purity >98 %
Description Potent TRPM8 antagonist (IC 50 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.
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Product References

Blockade of TRPM8 activity reduces the invasion potential of oral squamous - Blockade of TRPM8 activity reduces the invasion potential of oral squamous

Okamoto Y, Ohkubo T, Ikebe T, Yamazaki J. Int J Oncol. 2012 May;40(5):1431-40.

Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as - Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as

Ohmi M, Shishido Y, Inoue T, Ando K, Fujiuchi A, Yamada A, Watanabe S, Kawamura K. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8.