RQ 00203078

Key Product Details

Product Description

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.

Product Specifications for RQ 00203078

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for RQ 00203078

The following data is based on the product molecular weight 554.85.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.80 mL	9.01 mL	18.02 mL
5 mM	0.36 mL	1.80 mL	3.60 mL
10 mM	0.18 mL	0.90 mL	1.80 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 7 publications citing the usage of this product.

• Ohmi Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg.Med.Chem.Lett. 2014 PMID: 25455182
• Okamoto Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int.J.Oncol. 2012 PMID: 22267123

Product Documents for RQ 00203078